-
1
-
-
1542268206
-
Selective optimization of side activities: Another way for drug discovery
-
Wermuth, C. Selective optimization of side activities: another way for drug discovery. J. Med. Chem., 2004, 47, 1303-1314.
-
(2004)
J. Med. Chem
, vol.47
, pp. 1303-1314
-
-
Wermuth, C.1
-
2
-
-
0024239320
-
Methods for drug discovery: Development of potent, selective, orally effective Cholecystokinin antagonists
-
Evans, B.E.; Rittle, K.E.; Bock, M.G.; DiPardo, R.M.; Freidinger, R.M.; Whitter, W.L.; Lundell, G.F.; Veber, D.F.; Anderson, P.S.; Chang, R.S.L.; Lotti, V.J.; Cerino, D.J.; Chen, T.B.; Kling, P.J.; Kunkel, K.A.; Springer, J.P.; Hirshfield, J. Methods for drug discovery: development of potent, selective, orally effective Cholecystokinin antagonists. J. Med. Chem., 1988, 31, 2235-2246.
-
(1988)
J. Med. Chem.
, vol.31
, pp. 2235-2246
-
-
Evans, B.E.1
Rittle, K.E.2
Bock, M.G.3
DiPardo, R.M.4
Freidinger, R.M.5
Whitter, W.L.6
Lundell, G.F.7
Veber, D.F.8
Anderson, P.S.9
Chang, R.S.L.10
Lotti, V.J.11
Cerino, D.J.12
Chen, T.B.13
Kling, P.J.14
Kunkel, K.A.15
Springer, J.P.16
Hirshfield, J.17
-
3
-
-
6444230439
-
Lead generation: Showing the seeds for future success
-
Bleicher, K.H.; Nettekoven, M.; Peters, J.U.; Wyler, R. Lead generation: Showing the seeds for future success. Chimia, 2004, 58, 588-600.
-
(2004)
Chimia
, vol.58
, pp. 588-600
-
-
Bleicher, K.H.1
Nettekoven, M.2
Peters, J.U.3
Wyler, R.4
-
4
-
-
0037020329
-
Drug design strategies for targeting G-protein coupled receptors
-
Klabunde, T.; Hessler, G. Drug design strategies for targeting G-protein coupled receptors. ChemBiochem., 2002, 3, 928-944.
-
(2002)
ChemBiochem
, vol.3
, pp. 928-944
-
-
Klabunde, T.1
Hessler, G.2
-
5
-
-
4243159924
-
Privileged structures: Applications in drug design
-
DeSimone, R.W.; Currie, K.S.; Mitchell, S.A.; Darrow, J.W.; Pippin, D.A. Privileged structures: Applications in drug design. Comb. Chem. High Through. Screen., 2004, 7, 473-493.
-
(2004)
Comb. Chem. High Through. Screen.
, vol.7
, pp. 473-493
-
-
DeSimone, R.W.1
Currie, K.S.2
Mitchell, S.A.3
Darrow, J.W.4
Pippin, D.A.5
-
6
-
-
0029894013
-
The properties of known drugs. 1. Molecular frameworks
-
Bemis, G.W.; Murcko, M.A. The properties of known drugs. 1. Molecular frameworks. J. Med. Chem., 1996, 39, 2887-2893.
-
(1996)
J. Med. Chem.
, vol.39
, pp. 2887-2893
-
-
Bemis, G.W.1
Murcko, M.A.2
-
7
-
-
4344569207
-
The different strategies for designing GPCR and kinase targeted libraries
-
Lowrie, J.F.; Delisle, R.K.; Hobbs, D.W.; Diller, D.J. The different strategies for designing GPCR and kinase targeted libraries. Comb. Chem. High Through. Screen., 2004, 7, 495-510.
-
(2004)
Comb. Chem. High Through. Screen.
, vol.7
, pp. 495-510
-
-
Lowrie, J.F.1
Delisle, R.K.2
Hobbs, D.W.3
Diller, D.J.4
-
8
-
-
0037366605
-
The combinatorial synthesis of bicyclic privileged structures or privileged substructures
-
Horton, D.A.; Bourne, G.T.; Smythe, M.L. The combinatorial synthesis of bicyclic privileged structures or privileged substructures. Chem. Rev., 2003, 103, 893-930.
-
(2003)
Chem. Rev
, vol.103
, pp. 893-930
-
-
Horton, D.A.1
Bourne, G.T.2
Smythe, M.L.3
-
10
-
-
0042121318
-
Medicinal chemistry to target family-directed masterkeys
-
Muller, G. Medicinal chemistry to target family-directed masterkeys. Drug Discov Today, 2003, 8, 681-691.
-
(2003)
Drug Discov Today
, vol.8
, pp. 681-691
-
-
Muller, G.1
-
11
-
-
15444374352
-
2(3H)-benzoxazolone and bioisosters as "privileged scaffold" in the design of pharmacological probes
-
Poupaert, J.; Carato, P.; Colacillo, E. 2(3H)-benzoxazolone and bioisosters as "privileged scaffold" in the design of pharmacological probes. Curr. Med. Chem., 2005, 12, 877-885.
-
(2005)
Curr. Med. Chem.
, vol.12
, pp. 877-885
-
-
Poupaert, J.1
Carato, P.2
Colacillo, E.3
-
12
-
-
1642288258
-
Novel inhibitors of DNA gyrase: 3D structure based biased needle screening, hit validation by biophysical methods, and 3D guided optimization: A promising alternative to random screening
-
Boehm, H.-J.; Boehringer, M.; Bur, D.; Gmuender, H.; Huber, W.; Klaus, W.; Kostreva, D.; Kuehne, H.; Luebbers, T.; Meunier-Keller, N.; Mueller, F. Novel inhibitors of DNA gyrase: 3D structure based biased needle screening, hit validation by biophysical methods, and 3D guided optimization: a promising alternative to random screening. J. Med. Chem., 2000, 43, 2664-2674.
-
(2000)
J. Med. Chem
, vol.43
, pp. 2664-2674
-
-
Boehm, H.-J.1
Boehringer, M.2
Bur, D.3
Gmuender, H.4
Huber, W.5
Klaus, W.6
Kostreva, D.7
Kuehne, H.8
Luebbers, T.9
Meunier-Keller, N.10
Mueller, F.11
-
13
-
-
0842304428
-
Recognition of privileged structures by G-protein coupled receptors
-
Bondensgaart, K.; Ankerson, M.; Thogersen, H.; Hansen, B.S.; Wulff, B.S.; Bywater, R.P. Recognition of privileged structures by G-protein coupled receptors. J. Med. Chem., 2004, 47, 888-899.
-
(2004)
J. Med. Chem
, vol.47
, pp. 888-899
-
-
Bondensgaart, K.1
Ankerson, M.2
Thogersen, H.3
Hansen, B.S.4
Wulff, B.S.5
Bywater, R.P.6
-
14
-
-
17244370796
-
Over one hundred peptide-activated G protein coupled receptors recognize ligands with turn structure
-
Tyndall, J.D.A.; Pfeiffer, B.; Abbenante, G.; Fairlie, D.P. Over one hundred peptide-activated G protein coupled receptors recognize ligands with turn structure. Chem. Rev., 2005, 105, 793-826.
-
(2005)
Chem. Rev
, vol.105
, pp. 793-826
-
-
Tyndall, J.D.A.1
Pfeiffer, B.2
Abbenante, G.3
Fairlie, D.P.4
-
15
-
-
2942565810
-
Natural products and combinatorial chemistry: Back to the future
-
Ortholand, J.Y.; Ganesan, A. Natural products and combinatorial chemistry: back to the future. Curr. Opin. Chem. Biol., 2004, 8, 271-280.
-
(2004)
Curr. Opin. Chem. Biol
, vol.8
, pp. 271-280
-
-
Ortholand, J.Y.1
Ganesan, A.2
-
16
-
-
0033104653
-
Statistical investigation into the structural complementarity of natural products and synthetic compounds
-
Henkel, T.; Brunne, R.M.; Muller, H.; Reichel, F. Statistical investigation into the structural complementarity of natural products and synthetic compounds. Angew. Chem. Int. Engl., 1999, 38, 643-647.
-
(1999)
Angew. Chem. Int. Engl
, vol.38
, pp. 643-647
-
-
Henkel, T.1
Brunne, R.M.2
Muller, H.3
Reichel, F.4
-
17
-
-
11144311139
-
Lessons from natural molecules
-
Walsh, C.; Clardy, J. Lessons from natural molecules. Nature, 2004, 432, 829-837.
-
(2004)
Nature
, vol.432
, pp. 829-837
-
-
Walsh, C.1
Clardy, J.2
-
18
-
-
0037208308
-
Property distribution: Differences between drugs, natural products, and molecules from combinatorial chemistry
-
Feher, M.; Schmidt, J.M. Property distribution: differences between drugs, natural products, and molecules from combinatorial chemistry. J Chem. Inf. Comput. Sci., 2003, 43, 218-227.
-
(2003)
J Chem. Inf. Comput. Sci.
, vol.43
, pp. 218-227
-
-
Feher, M.1
Schmidt, J.M.2
-
19
-
-
28444498830
-
Charting biologically relevant chemical space: A structural classification of natural products (SCONP)
-
Koch, M.A.; Shuffenhauer, A.; Scheck, M.; Wetzel, S.; Casaulta, M.; Odermatt, A.; Ertl, P.; Waldmann, H. Charting biologically relevant chemical space: a structural classification of natural products (SCONP). Proc. Natl. Acad Sci. USA, 2005, 102, 17272-17277.
-
(2005)
Proc. Natl. Acad Sci. USA
, vol.102
, pp. 17272-17277
-
-
Koch, M.A.1
Shuffenhauer, A.2
Scheck, M.3
Wetzel, S.4
Casaulta, M.5
Odermatt, A.6
Ertl, P.7
Waldmann, H.8
-
20
-
-
33846871027
-
The scaffold tree-Visualization of the scaffold universe by hierarchical scaffold classification
-
Schuffenhauer, A.; Ertl, P.; Roggo, S.; Wetzel, S.; Koch, M.A.; Waldmann, H. The scaffold tree-Visualization of the scaffold universe by hierarchical scaffold classification. J. Chem. Inf. Model., 2007, 47, 47-58.
-
(2007)
J. Chem. Inf. Model
, vol.47
, pp. 47-58
-
-
Schuffenhauer, A.1
Ertl, P.2
Roggo, S.3
Wetzel, S.4
Koch, M.A.5
Waldmann, H.6
-
21
-
-
10044253102
-
-
Koch, M.A.; Wittenberg, L.O.; Basu, S.; Jeyaraj, D.A.; Gourzoulidou, E.; Reinecke, K.; Odermatt, A.; Waldmann, H. Proc. Natl. Acad. Sci. USA, 2004, 101, 16721-16726.
-
(2004)
Proc. Natl. Acad. Sci. USA
, vol.101
, pp. 16721-16726
-
-
Koch, M.A.1
Wittenberg, L.O.2
Basu, S.3
Jeyaraj, D.A.4
Gourzoulidou, E.5
Reinecke, K.6
Odermatt, A.7
Waldmann, H.8
-
22
-
-
33845306506
-
Protein structure similarity clustering: Dynamic treatment of PDB structures facilitates clustering
-
Charette, B.D.; MacDonald, R.G.; Wetzel, S.; Berkowitz, D.B.; Waldmann, H. Protein structure similarity clustering: dynamic treatment of PDB structures facilitates clustering. Angew. Chem. Int. Engl., 2006, 45, 7766-7770.
-
(2006)
Angew. Chem. Int. Engl.
, vol.45
, pp. 7766-7770
-
-
Charette, B.D.1
McDonald, R.G.2
Wetzel, S.3
Berkowitz, D.B.4
Waldmann, H.5
-
23
-
-
33746047675
-
Discovery of protein phosphatase inhibitor classes by biology-oriented synthesis
-
Noren-Muller, A.; Reis-Correa, I.; Prinz, H.; Rosenbaum, C.; Saxena, K.; Schwalbe, H.J.; Vestweber, D.; Cagna, G.; Schunk, S.; Schwarz, O.; Schieve, H.; Waldmann, H. Discovery of protein phosphatase inhibitor classes by biology-oriented synthesis. Proc. Natl. Acad. Sci. USA, 2006, 103, 10606-10611.
-
(2006)
Proc. Natl. Acad. Sci. USA
, vol.103
, pp. 10606-10611
-
-
Noren-Muller, A.1
Reis-Correa, I.2
Prinz, H.3
Rosenbaum, C.4
Saxena, K.5
Schwalbe, H.J.6
Vestweber, D.7
Cagna, G.8
Schunk, S.9
Schwarz, O.10
Schieve, H.11
Waldmann, H.12
-
24
-
-
42249106818
-
Synthesis of a dysidiolide-inspired compound library and discovery of acetylcholinesterase inhibitors based on protein structure similarity clustering (PSSC)
-
Scheck, M.; Koch, M.A.; Waldmann, H. Synthesis of a dysidiolide-inspired compound library and discovery of acetylcholinesterase inhibitors based on protein structure similarity clustering (PSSC). Tetrahedron, 2008, 64, 4792-4802.
-
(2008)
Tetrahedron
, vol.64
, pp. 4792-4802
-
-
Scheck, M.1
Koch, M.A.2
Waldmann, H.3
-
25
-
-
67649341990
-
From fragment to clinical candidate-a historical perspective
-
Chessari, G.; Woodhead, A.J. From fragment to clinical candidate-a historical perspective. Drug Discov. Today, 2009, 14, 668-675.
-
(2009)
Drug Discov. Today
, vol.14
, pp. 668-675
-
-
Chessari, G.1
Woodhead, A.J.2
-
26
-
-
3042689621
-
Fragment-based drug discovery
-
Erlanson, D.A.; McDowell, R.S.; O'Brien, T. Fragment-based drug discovery. J. Med. Chem., 2004, 47, 3463-3482.
-
(2004)
J. Med. Chem
, vol.47
, pp. 3463-3482
-
-
Erlanson, D.A.1
McDowell, R.S.2
O'Brien, T.3
-
27
-
-
33645422011
-
Are target-family-privileged substructures truly privileged?
-
Schnur, D.M.; Hermsmeier, M.A.; Tebben, A.J. Are target-family-privileged substructures truly privileged? J. Med. Chem., 2006, 49, 2000-2009.
-
(2006)
J. Med. Chem
, vol.49
, pp. 2000-2009
-
-
Schnur, D.M.1
Hermsmeier, M.A.2
Tebben, A.J.3
-
28
-
-
41649105837
-
Kinase-likeness and kinase-privileged fragments: Toward virtual polypharmacology
-
Aronov, A.M.; McClain, B.; Moody, C.S.; Murcko, M.A. Kinase-likeness and kinase-privileged fragments: toward virtual polypharmacology. J. Med. Chem., 2008, 51, 1214-1222.
-
(2008)
J. Med. Chem
, vol.51
, pp. 1214-1222
-
-
Aronov, A.M.1
McClain, B.2
Moody, C.S.3
Murcko, M.A.4
-
29
-
-
33646258711
-
Mining a chemical database for fragment co-occurrence: Discovery of "Chemical Clichès"
-
Lameijer, E.; Kok, J.N.; Back, T.; Ijzerman, A.P. Mining a chemical database for fragment co-occurrence: discovery of "Chemical Clichès". J. Chem. Inf. Model., 2007 46, 553-562.
-
(2007)
J. Chem. Inf. Model
, vol.46
, pp. 553-562
-
-
Lameijer, E.1
Kok, J.N.2
Back, T.3
Ijzerman, A.P.4
-
30
-
-
42949088496
-
Chemical fragments as foundations for understanding target space and activity prediction
-
Sutherland, J.J.; Higgs, R.E.; Watson, I.; Vieth, M. Chemical fragments as foundations for understanding target space and activity prediction. J. Med. Chem., 2008, 51, 2689-2700.
-
(2008)
J. Med. Chem.
, vol.51
, pp. 2689-2700
-
-
Sutherland, J.J.1
Higgs, R.E.2
Watson, I.3
Vieth, M.4
-
31
-
-
51849102040
-
Formal concept analysis for the identification of molecular fragment combinations specific for active and highly potent compounds
-
Lounkine, E.; Auer, J.; Bajorath, J. Formal concept analysis for the identification of molecular fragment combinations specific for active and highly potent compounds. J. Med. Chem., 2008, 51, 5342-5348.
-
(2008)
J. Med. Chem
, vol.51
, pp. 5342-5348
-
-
Lounkine, E.1
Auer, J.2
Bajorath, J.3
-
32
-
-
77249139237
-
Systematic analysis of public domain compound potency data identifies selective molecular scaffolds across druggable target families
-
Hu, Y.; Wassermann, A.M.; Lounkine, E.; Bajorath, J. Systematic analysis of public domain compound potency data identifies selective molecular scaffolds across druggable target families. J. Med. Chem., 2010, 53, 752-758.
-
(2010)
J. Med. Chem
, vol.53
, pp. 752-758
-
-
Hu, Y.1
Wassermann, A.M.2
Lounkine, E.3
Bajorath, J.4
-
33
-
-
0037119336
-
From protein domains to drug candidates: Natural products as guiding principles in the design and synthesis of compound libraries
-
Breinbauer, R.; Vetter, I.R.; Waldmann, H. From protein domains to drug candidates: Natural products as guiding principles in the design and synthesis of compound libraries. Angew. Chem. Int. Engl., 2002, 41, 2878-2890.
-
(2002)
Angew. Chem. Int. Engl.
, vol.41
, pp. 2878-2890
-
-
Breinbauer, R.1
Vetter, I.R.2
Waldmann, H.3
-
34
-
-
0141828504
-
Protein structure similarity as guiding principle for combinatorial library design
-
Koch, M.A.; Breinbauer, R.; Waldmann, H. Protein structure similarity as guiding principle for combinatorial library design. Biol. Chem., 2003, 384, 1265-1272.
-
(2003)
Biol. Chem
, vol.384
, pp. 1265-1272
-
-
Koch, M.A.1
Breinbauer, R.2
Waldmann, H.3
-
35
-
-
0037057558
-
Design and pharmacology of N-[(3R)-1,2,3,4-tetrahydroisoquinolinium-3-ylcarbonyl]-(1R)-1-(4-chlorobenzyl)-2-[4-cyclohexyl-4-(1H-1,2,4-triazol-1-ylmethyl)piperidin-1-yl]-2-oxoethylamine (1), a potent, selective, melanocortin subtype-4 receptor agonist
-
Sebhat, I.K.; Martin, W.J.; Ye, Z.; Barakat, K.; Mosley, R.T.; Johnston, D.B.R.; Bakshi, R.; Palucki, B.; Weinberg, D.H.; MacNeil, T.; Kalyani, R.N.; Tang, R.; Stearns, R.A.; Miller, R.R.; Tanvakopoulos, C.; Strack, A.M.; McGowan, E.; Cashen, D.E.; Drisko, J.E.; Hom, G.J.; Howard, A.D.; MacIntyre, E.; van der Ploeg, L.H.T.; Patchett, A.A.; Nargund, R.P. Design and pharmacology of N-[(3R)-1,2,3,4-tetrahydroisoquinolinium-3-ylcarbonyl]-(1R)-1-(4-chlorobenzyl)-2-[4-cyclohexyl-4-(1H-1,2,4-triazol-1-ylmethyl)piperidin-1-yl]-2-oxoethylamine (1), a potent, selective, melanocortin subtype-4 receptor agonist J. Med. Chem., 2002, 45, 4589-4593.
-
(2002)
J. Med. Chem.
, vol.45
, pp. 4589-4593
-
-
Sebhat, I.K.1
Martin, W.J.2
Ye, Z.3
Barakat, K.4
Mosley, R.T.5
Johnston, D.B.R.6
Bakshi, R.7
Palucki, B.8
Weinberg, D.H.9
McNeil, T.10
Kalyani, R.N.11
Tang, R.12
Stearns, R.A.13
Miller, R.R.14
Tanvakopoulos, C.15
Strack, A.M.16
McGowan, E.17
Cashen, D.E.18
Drisko, J.E.19
Hom, G.J.20
Howard, A.D.21
McIntyre, E.22
van der Ploeg, L.H.T.23
Patchett, A.A.24
Nargund, R.P.25
more..
-
36
-
-
5144234838
-
Piperazinebenzylamines as potent and selective antagonists of the human melanocortin-4 receptor
-
Pontillo, J.; Tran, J.A.; Fleck, B.A.; Marinkovic, D.; Arellano, M.; Tucci, F.C.; Lanier, M.; Nelson, J.; Parker, J.; Saunders, J.; Murphy, B.; Foster, A.C.; Chen, C. Piperazinebenzylamines as potent and selective antagonists of the human melanocortin-4 receptor. Bioorg. Med. Chem. Lett., 2004, 14, 5605-5609.
-
(2004)
Bioorg. Med. Chem. Lett
, vol.14
, pp. 5605-5609
-
-
Pontillo, J.1
Tran, J.A.2
Fleck, B.A.3
Marinkovic, D.4
Arellano, M.5
Tucci, F.C.6
Lanier, M.7
Nelson, J.8
Parker, J.9
Saunders, J.10
Murphy, B.11
Foster, A.C.12
Chen, C.13
-
37
-
-
25844475958
-
Privileged structure based ligands for melanocortin receptors-substituted benzylic piperazine derivatives
-
Fisher, M.J.; Backer, R.T.; Collado, I.; de Frutos, O.; Husain, S.; Hsiung, H.M.; Kuklish, S.L.; Mateo, A.I.; Mullaney, J.T.; Ornstein, P.L.; Paredes, C.G.; O'Brian, T.P.; Richardson, T.I.; Shah, J.; Zgombick, J.M.; Briner, K. Privileged structure based ligands for melanocortin receptors-substituted benzylic piperazine derivatives. Bioorg. Med. Chem. Lett., 2005, 15, 4973-4978.
-
(2005)
Bioorg. Med. Chem. Lett
, vol.15
, pp. 4973-4978
-
-
Fisher, M.J.1
Backer, R.T.2
Collado, I.3
de Frutos, O.4
Husain, S.5
Hsiung, H.M.6
Kuklish, S.L.7
Mateo, A.I.8
Mullaney, J.T.9
Ornstein, P.L.10
Paredes, C.G.11
O'Brian, T.P.12
Richardson, T.I.13
Shah, J.14
Zgombick, J.M.15
Briner, K.16
-
38
-
-
24344485148
-
Privileged structure-based ligands for melanocortin receptorstetrahydroquinolines, indoles, and aminotetralines
-
Fisher, M.J.; Backer, R.T.; Husain, S.; Hsiung, H.M.; Mullaney, J.T.; O'Brian, T.P.; Ornstein, P.L.; Rothhaar, R.R.; Zgombick, J.M.; Briner, K. Privileged structure-based ligands for melanocortin receptorstetrahydroquinolines, indoles, and aminotetralines. Bioorg. Med. Chem. Lett., 2005, 15, 4459-4462.
-
(2005)
Bioorg. Med. Chem. Lett
, vol.15
, pp. 4459-4462
-
-
Fisher, M.J.1
Backer, R.T.2
Husain, S.3
Hsiung, H.M.4
Mullaney, J.T.5
O'Brian, T.P.6
Ornstein, P.L.7
Rothhaar, R.R.8
Zgombick, J.M.9
Briner, K.10
-
39
-
-
9144220758
-
Synthesis and structure-activity relationships of novel arylpiperazines as potent and selective agonists of the melanocortin subtype-4 receptor
-
Richardson, T.I.; Ornstein, P.L.; Briner, K.; Fisher, M.J.; Backer, R.T.; Biggers, K.; Clay, M.P.; Emmerson, P.J.; Hertel, L.W.; Hsiung, H.M.; Husain, S.; Kahl, S.D.; Lee, J.A.; Lindstrom, T.D.; Martinelli, M.J.; Mayer, J.P.; Mullaney, J.T.; O'Brien, T.P.; Pawlak, J.M.; Revell, K.D.; Shah, J.; Zgombick, J.M.; Herr, R.J.; Melekhov, A.; Sampson, P.B.; King, C.H.R. Synthesis and structure-activity relationships of novel arylpiperazines as potent and selective agonists of the melanocortin subtype-4 receptor. J. Med. Chem., 2004, 47, 744-755.
-
(2004)
J. Med. Chem
, vol.47
, pp. 744-755
-
-
Richardson, T.I.1
Ornstein, P.L.2
Briner, K.3
Fisher, M.J.4
Backer, R.T.5
Biggers, K.6
Clay, M.P.7
Emmerson, P.J.8
Hertel, L.W.9
Hsiung, H.M.10
Husain, S.11
Kahl, S.D.12
Lee, J.A.13
Lindstrom, T.D.14
Martinelli, M.J.15
Mayer, J.P.16
Mullaney, J.T.17
O'Brien, T.P.18
Pawlak, J.M.19
Revell, K.D.20
Shah, J.21
Zgombick, J.M.22
Herr, R.J.23
Melekhov, A.24
Sampson, P.B.25
King, C.H.R.26
more..
-
40
-
-
33746502556
-
Privileged structure based ligands for melanocortin receptors-4,4-disubstituted piperidine derivatives
-
Kuklish, S.L.; Backer, R.T.; Briner, K.; Doecke, C.W.; Husain, S.; Mullaney, J.T.; Ornstein, P.L.; Zgombick, J.M.; O'Brien, T.P.; Fisher, M.J. Privileged structure based ligands for melanocortin receptors-4,4-disubstituted piperidine derivatives. Bioorg. Med. Chem. Lett., 2006, 16, 3843-3846.
-
(2006)
Bioorg. Med. Chem. Lett
, vol.16
, pp. 3843-3846
-
-
Kuklish, S.L.1
Backer, R.T.2
Briner, K.3
Doecke, C.W.4
Husain, S.5
Mullaney, J.T.6
Ornstein, P.L.7
Zgombick, J.M.8
O'Brien, T.P.9
Fisher, M.J.10
-
41
-
-
33746636462
-
Privileged structure based ligands for melanocortin 4-receptors-aliphatic piperazine derivatives
-
Briner, K.; Collado, I.; Fisher, M.J.; Garcia-Paredes, C.; Husain, S.; Kuklish, S.L.; Mateo, A.I.; O'Brien, T.P.; Ornstein, P.L.; Zgombick, J.; de Frutos, O. Privileged structure based ligands for melanocortin 4-receptors-aliphatic piperazine derivatives. Bioorg. Med. Chem. Lett. 2006, 16, 3449-3453.
-
(2006)
Bioorg. Med. Chem. Lett
, vol.16
, pp. 3449-3453
-
-
Briner, K.1
Collado, I.2
Fisher, M.J.3
Garcia-Paredes, C.4
Husain, S.5
Kuklish, S.L.6
Mateo, A.I.7
O'Brien, T.P.8
Ornstein, P.L.9
Zgombick, J.10
de Frutos, O.11
-
42
-
-
0037006785
-
Natural product derived receptor tyrosine kinase inhibitors: Identification of IGF-1R, Tie-2 and VEGFR-3 inhibitors
-
Stahl, P.; Kissau, L.; Mazitschek, R.; Giannis, A.; Waldmann, H. Natural product derived receptor tyrosine kinase inhibitors: identification of IGF-1R, Tie-2 and VEGFR-3 inhibitors. Angew. Chem. Int. Engl., 2002, 41, 1174-1178.
-
(2002)
Angew. Chem. Int. Engl
, vol.41
, pp. 1174-1178
-
-
Stahl, P.1
Kissau, L.2
Mazitschek, R.3
Giannis, A.4
Waldmann, H.5
-
43
-
-
0035952261
-
Initial structure-activity relationship of a novel class of nonpeptidyl GnRH receptor antagonists: 2-arylindoles
-
Chu, L.; Hutchins, J.E.; Weber, A.E.; Lo, J.L.; Yang, Y.T.; Cheng, K.; Smith, R.G.; Fisher, M.H.; Wyvratt, M.J.; Goulet, M.T. Initial structure-activity relationship of a novel class of nonpeptidyl GnRH receptor antagonists: 2-arylindoles. Bioorg. Med. Chem. Lett., 2001, 11, 509-513.
-
(2001)
Bioorg. Med. Chem. Lett.
, vol.11
, pp. 509-513
-
-
Chu, L.1
Hutchins, J.E.2
Weber, A.E.3
Lo, J.L.4
Yang, Y.T.5
Cheng, K.6
Smith, R.G.7
Fisher, M.H.8
Wyvratt, M.J.9
Goulet, M.T.10
-
44
-
-
0035952296
-
SAR studies of novel 5-substituted 2-arylindoles as nonpeptidyl GnRH receptor antagonists
-
Chu, L.; Lo, J.L.; Yang, Y.T.; Cheng, K.; Smith, R.G.; Fisher, M.H.; Wyvratt, M.J.; Goulet, M.T. SAR studies of novel 5-substituted 2-arylindoles as nonpeptidyl GnRH receptor antagonists. Bioorg. Med. Chem. Lett., 2001, 11, 515-517.
-
(2001)
Bioorg. Med. Chem. Lett
, vol.11
, pp. 515-517
-
-
Chu, L.1
Lo, J.L.2
Yang, Y.T.3
Cheng, K.4
Smith, R.G.5
Fisher, M.H.6
Wyvratt, M.J.7
Goulet, M.T.8
-
45
-
-
0034684780
-
Solid-phase synthesis of 2,3-disubstituted indoles: Discovery of a novel, high-affinity, selective h5-HT2A antagonist
-
Smith, A.L.; Stevenson, G.I.; Lewis, S.; Patel, S.; Castro, J.L. Solid-phase synthesis of 2,3-disubstituted indoles: discovery of a novel, high-affinity, selective h5-HT2A antagonist. Bioorg. Med. Chem. Lett., 2000, 10, 2693-2696.
-
(2000)
Bioorg. Med. Chem. Lett
, vol.10
, pp. 2693-2696
-
-
Smith, A.L.1
Stevenson, G.I.2
Lewis, S.3
Patel, S.4
Castro, J.L.5
-
46
-
-
18244382828
-
Combinatorial synthesis of 3-(amidoalkyl) and 3-(aminoalkyl)-2-arylindole derivatives: Discovery of potent ligands for a variety of G-protein coupled receptors
-
Willoughby, C.A.; Hutchins, S.M.; Rosauer, K.G.; Dhar, M.J.; Chapman, K.T.; Chicchi, G.G.; Sadowski, S.; Weinberg, D.H.; Patel, S.; Malkowitz, L.; Di Salvo, J.; Pacholok, S.G.; Cheng, K. Combinatorial synthesis of 3-(amidoalkyl) and 3-(aminoalkyl)-2-arylindole derivatives: discovery of potent ligands for a variety of G-protein coupled receptors. Bioorg. Med. Chem. Lett., 2002, 12, 93-96.
-
(2002)
Bioorg. Med. Chem. Lett
, vol.12
, pp. 93-96
-
-
Willoughby, C.A.1
Hutchins, S.M.2
Rosauer, K.G.3
Dhar, M.J.4
Chapman, K.T.5
Chicchi, G.G.6
Sadowski, S.7
Weinberg, D.H.8
Patel, S.9
Malkowitz, L.10
Di Salvo, J.11
Pacholok, S.G.12
Cheng, K.13
-
47
-
-
0032561511
-
Rapid identification of subtype-selective agonists of the somatostatin receptor through combinatorial chemistry
-
Roher, S.P.; Birzin, E.T.; Mosley, R.T.; Berk, S.C.; Hutchins, S.M.; Shen, D.M.; Xiong, Y.X.; Hayes, E.C.; Parmar, R.M.; Foor, F.; Mitra, S.W.; Degrado, S.J.; Shu, M.; Klopp, J.M.; Cai, S.J.; Blake, A.; Chan, W.W.S.; Pasternak, A.; Yang, L.Y.; Patchett, A.A.; Smith, R.G.; Chapman, K.T.; Schaeffer, J.M. Rapid identification of subtype-selective agonists of the somatostatin receptor through combinatorial chemistry. Science, 1998, 282, 737-740.
-
(1998)
Science
, vol.282
, pp. 737-740
-
-
Roher, S.P.1
Birzin, E.T.2
Mosley, R.T.3
Berk, S.C.4
Hutchins, S.M.5
Shen, D.M.6
Xiong, Y.X.7
Hayes, E.C.8
Parmar, R.M.9
Foor, F.10
Mitra, S.W.11
Degrado, S.J.12
Shu, M.13
Klopp, J.M.14
Cai, S.J.15
Blake, A.16
Chan, W.W.S.17
Pasternak, A.18
Yang, L.Y.19
Patchett, A.A.20
Smith, R.G.21
Chapman, K.T.22
Schaeffer, J.M.23
more..
-
48
-
-
0028245052
-
Design of orally active, non-peptidic inhibitors of human leucocyte elastase
-
Brown, F.J.; Andisik, D.W.; Bernstein, P.R.; Bryant, C.B.; Ceccarelli, C.; Damewood, J.R.; Edwards, P.D.; Earley, R.A.; Feeney, S.; Green, R.C.; Gomes, B.; Kosmider, B.J.; Krell, R.D.; Shaw, A.; Steelman, G.B.; Thomas, R.M.; Vacek, E.P.; Veale, C.A.; Tuthill, P.A.; Warner, P.; Williams, J.C.; Wolanin, D.J.; Woolson, S.A. Design of orally active, non-peptidic inhibitors of human leucocyte elastase. J. Med. Chem., 1994, 37, 1259-1261.
-
(1994)
J. Med. Chem.
, vol.37
, pp. 1259-1261
-
-
Brown, F.J.1
Andisik, D.W.2
Bernstein, P.R.3
Bryant, C.B.4
Ceccarelli, C.5
Damewood, J.R.6
Edwards, P.D.7
Earley, R.A.8
Feeney, S.9
Green, R.C.10
Gomes, B.11
Kosmider, B.J.12
Krell, R.D.13
Shaw, A.14
Steelman, G.B.15
Thomas, R.M.16
Vacek, E.P.17
Veale, C.A.18
Tuthill, P.A.19
Warner, P.20
Williams, J.C.21
Wolanin, D.J.22
Woolson, S.A.23
more..
-
49
-
-
0027945808
-
Nonpeptidic inhibitors of human leucocyte elastase. 3. Design, synthesis, X-rays crystallographic analysis, and structure-activity relationships for a series of orally active 3-amino-6-phenyl-2-pyridinyl trifluoromethyl ketones
-
Bernstein, P.R.; Andisik, D.; Bradley, P.K.; Bryant, C.B.; Ceccarelli, C.; Damewood, J.R.; Earley, R.; Edwards, P.D.; Feeney, S.; Gomes, B.C.; Kosmider, B.J.; Steelman, G.B.; Thomas, R.M.; Vacek, E.P.; Veale, C.A.; Williams, J.C.; Wolanin, D.J.; Woolson, S.A. Nonpeptidic inhibitors of human leucocyte elastase. 3. Design, synthesis, X-rays crystallographic analysis, and structure-activity relationships for a series of orally active 3-amino-6-phenyl-2-pyridinyl trifluoromethyl ketones. J. Med. Chem., 1994, 37, 3313-3326.
-
(1994)
J. Med. Chem
, vol.37
, pp. 3313-3326
-
-
Bernstein, P.R.1
Andisik, D.2
Bradley, P.K.3
Bryant, C.B.4
Ceccarelli, C.5
Damewood, J.R.6
Earley, R.7
Edwards, P.D.8
Feeney, S.9
Gomes, B.C.10
Kosmider, B.J.11
Steelman, G.B.12
Thomas, R.M.13
Vacek, E.P.14
Veale, C.A.15
Williams, J.C.16
Wolanin, D.J.17
Woolson, S.A.18
-
50
-
-
0029008367
-
Nonpeptidic inhibitors of human leukocyte elastase. 5: Design, synthesis, and X-ray crystallography of a series of orally active 5-aminopyrimidin-6-one-containing trifluoromethylketones
-
Veale, C.A.; Bernstein, P.R.; Bryant, C.; Ceccarelli, C.; Damewood, J.R.; Earley, R.; Feeney, S.W.; Gomes, B.; Kosmider, B.J.; Steelman, G.B.; Thomas, R.M.; Vacek, E.P.; Williams, J.C.; Wolanin, D.J.; Woolson, S. Nonpeptidic inhibitors of human leukocyte elastase. 5: design, synthesis, and X-ray crystallography of a series of orally active 5-aminopyrimidin-6-one-containing trifluoromethylketones. J. Med. Chem., 1995, 38, 98-108.
-
(1995)
J. Med. Chem
, vol.38
, pp. 98-108
-
-
Veale, C.A.1
Bernstein, P.R.2
Bryant, C.3
Ceccarelli, C.4
Damewood, J.R.5
Earley, R.6
Feeney, S.W.7
Gomes, B.8
Kosmider, B.J.9
Steelman, G.B.10
Thomas, R.M.11
Vacek, E.P.12
Williams, J.C.13
Wolanin, D.J.14
Woolson, S.15
-
51
-
-
17044421362
-
Protein structure similarity clustering and natural product structure as guiding principles in drug discovery
-
Koch, M.A.; Waldmann, H. Protein structure similarity clustering and natural product structure as guiding principles in drug discovery. Drug Discov Today, 2005, 10, 471-483.
-
(2005)
Drug Discov Today
, vol.10
, pp. 471-483
-
-
Koch, M.A.1
Waldmann, H.2
-
52
-
-
0037665145
-
Roscovitine and other purines as kinase inhibitors: From starfish oocytes to clinical trials
-
Meijer, L.; Raymond, E. Roscovitine and other purines as kinase inhibitors: from starfish oocytes to clinical trials. Acc. Chem. Res., 2003, 36, 417-425.
-
(2003)
Acc. Chem. Res
, vol.36
, pp. 417-425
-
-
Meijer, L.1
Raymond, E.2
-
53
-
-
0028093182
-
Inhibition of cyclin-dependent kinases by purine analogs
-
Vesely, J.; Havlicek, L.; Strnad, M.; Blow, J.J.; Donella-Deana, A.; Pinna, L.; Letham, D.S.; Kato, J.Y.; Detivaud, L.; Leclerc, S., Meijer, L. Inhibition of cyclin-dependent kinases by purine analogs. Eur. J. Biochem., 1994, 224, 771-786.
-
(1994)
Eur. J. Biochem
, vol.224
, pp. 771-786
-
-
Vesely, J.1
Havlicek, L.2
Strnad, M.3
Blow, J.J.4
Donella-Deana, A.5
Pinna, L.6
Letham, D.S.7
Kato, J.Y.8
Detivaud, L.9
Leclerc, S.10
Meijer, L.11
-
54
-
-
0034599655
-
Discovery of carbohydrate sulfotransferase inhibitors from a kinase-directed library
-
Armstrong, J.I.; Portley, A.R.; Chang, Y.T.; Nierengarten, D.M.; Cook, B.N.; Bowman, K.G.; Bishop, A.; Gray, N.S.; Shokat, K.M.; Schultz, P.G.; Bertozzi, C.R. Discovery of carbohydrate sulfotransferase inhibitors from a kinase-directed library. Angew. Chem. Int. Engl., 2000, 39, 1303-1306.
-
(2000)
Angew. Chem. Int. Engl
, vol.39
, pp. 1303-1306
-
-
Armstrong, J.I.1
Portley, A.R.2
Chang, Y.T.3
Nierengarten, D.M.4
Cook, B.N.5
Bowman, K.G.6
Bishop, A.7
Gray, N.S.8
Shokat, K.M.9
Schultz, P.G.10
Bertozzi, C.R.11
-
55
-
-
0035899193
-
Discovery of estrogen sulfotransferase inhibitors from a purine library screen
-
Verdugo, D.E.; Cancilla, M.T.; Ge, X.; Gray, N.S.; Chang, Y.T.; Schultz, P.G.; Negishi, M.; Leary, J.A.; Bertozzi, C.R. Discovery of estrogen sulfotransferase inhibitors from a purine library screen. J. Med. Chem., 2001, 44, 2683-2686.
-
(2001)
J. Med. Chem
, vol.44
, pp. 2683-2686
-
-
Verdugo, D.E.1
Cancilla, M.T.2
Ge, X.3
Gray, N.S.4
Chang, Y.T.5
Schultz, P.G.6
Negishi, M.7
Leary, J.A.8
Bertozzi, C.R.9
-
56
-
-
4544387724
-
Rapid discovery of potent sulfotransferase inhibitors by diversity-oriented reaction in microplates followed by in situ screening
-
Best, M.D.; Brick, A.; Chapman, E.; Lu, L.V.; Cheng, W.C.; Wong, C.H. Rapid discovery of potent sulfotransferase inhibitors by diversity-oriented reaction in microplates followed by in situ screening. ChemBiochem., 2004, 5, 811-819.
-
(2004)
ChemBiochem
, vol.5
, pp. 811-819
-
-
Best, M.D.1
Brick, A.2
Chapman, E.3
Lu, L.V.4
Cheng, W.C.5
Wong, C.H.6
-
57
-
-
0034555871
-
Development of an efficient, region-and stereoselective route to libraries based on the ll-D-glucose scaffold
-
Hirschmann, R.; Ducry, L.; Smith, A.B. Development of an efficient, region-and stereoselective route to libraries based on the ll-D-glucose scaffold. J. Org. Chem., 2000, 65, 8307-8316.
-
(2000)
J. Org. Chem.
, vol.65
, pp. 8307-8316
-
-
Hirschmann, R.1
Ducry, L.2
Smith, A.B.3
-
58
-
-
0034687226
-
Synthesis, of a Substance P antagonist with a Somatostatin scaffold: Factors affecting agonism/antagonism at the GPCRs and the role of pseudosymmetry
-
Liu, J.; Underwood, D.J.; Cascieri, M.A.; Rohrer, S.P.; Cantin, L.D.; Chicchi, G.; Smith, A.B.; Hirschmann, R. Synthesis, of a Substance P antagonist with a Somatostatin scaffold: factors affecting agonism/antagonism at the GPCRs and the role of pseudosymmetry. J. Med. Chem., 2000, 53, 3827-3831.
-
(2000)
J. Med. Chem
, vol.53
, pp. 3827-3831
-
-
Liu, J.1
Underwood, D.J.2
Cascieri, M.A.3
Rohrer, S.P.4
Cantin, L.D.5
Chicchi, G.6
Smith, A.B.7
Hirschmann, R.8
-
59
-
-
0027857964
-
De novo design and synthesis of Somatostatin non-peptide peptidomimetics utilizing oo-D-glucose as a novel scaffold
-
Hirschmann, R.; Nicolaou, K.C.; Pietranico, S.; Leahy, E.N.M.; Salvino, J.; Arison, B.; Cichy, M.A.; Spoors, P.G.; Shakespeare, W.C.; Sprengeler, P.A.; Hamley, P.; Smith, A.B.; Reisine, T.; Raynor, K.; Maechler, L.; Donaldson, C.; Vale, W.; Freidinger, R.M.; Cascieri, M.R.; Strader, C.D. De novo design and synthesis of Somatostatin non-peptide peptidomimetics utilizing oo-D-glucose as a novel scaffold. J. Am. Chem. Soc., 1993, 115, 12550-12568.
-
(1993)
J. Am. Chem. Soc
, vol.115
, pp. 12550-12568
-
-
Hirschmann, R.1
Nicolaou, K.C.2
Pietranico, S.3
Leahy, E.N.M.4
Salvino, J.5
Arison, B.6
Cichy, M.A.7
Spoors, P.G.8
Shakespeare, W.C.9
Sprengeler, P.A.10
Hamley, P.11
Smith, A.B.12
Reisine, T.13
Raynor, K.14
Maechler, L.15
Donaldson, C.16
Vale, W.17
Freidinger, R.M.18
Cascieri, M.R.19
Strader, C.D.20
more..
-
60
-
-
15444347630
-
Modulation of receptor and receptor subtype affinities using diastereomeric and enantiomeric monosaccharide scaffolds as a mean to structural and biological diversity: A new route to ether synthesis
-
Hirschmann, R.; Hynes, J.; Cichy-Knight, M.A.; van Rijn, R.D.; Sprengeler, P.A.; Spoors, P.G.; Shakespeare, W.C.; Pietranico-Cole, S.; Barbosa, J.; Liu, J.; Yao, W.; Rohrer, S.; Smith, A.B. Modulation of receptor and receptor subtype affinities using diastereomeric and enantiomeric monosaccharide scaffolds as a mean to structural and biological diversity: a new route to ether synthesis. J. Med. Chem., 1998, 41, 1382-1391.
-
(1998)
J. Med. Chem
, vol.41
, pp. 1382-1391
-
-
Hirschmann, R.1
Hynes, J.2
Cichy-Knight, M.A.3
van Rijn, R.D.4
Sprengeler, P.A.5
Spoors, P.G.6
Shakespeare, W.C.7
Pietranico-Cole, S.8
Barbosa, J.9
Liu, J.10
Yao, W.11
Rohrer, S.12
Smith, A.B.13
-
61
-
-
0026470597
-
Nonpeptidal peptidomimetics with pp-D-glucose scaffolding. A partial Somatostatin agonist bearing a close structural relationship to a potent, selective substance P antagonist
-
Hirschmann, R.; Nicolaou, K.C.; Pietranico S.; Savino, J.; Leahy, E.M.; Sprengler, P.A.; Furst, G.; Smith, A.B.; Strader, C.D.; Cascieri, M.A.; Candelore, M.R.; Donaldson, C.; Vale, W.; Maechler, L. Nonpeptidal peptidomimetics with pp-D-glucose scaffolding. A partial Somatostatin agonist bearing a close structural relationship to a potent, selective substance P antagonist. J. Am. Chem. Soc., 1992, 114, 9217-9218.
-
(1992)
J. Am. Chem. Soc
, vol.114
, pp. 9217-9218
-
-
Hirschmann, R.1
Nicolaou, K.C.2
Pietranico, S.3
Savino, J.4
Leahy, E.M.5
Sprengler, P.A.6
Furst, G.7
Smith, A.B.8
Strader, C.D.9
Cascieri, M.A.10
Candelore, M.R.11
Donaldson, C.12
Vale, W.13
Maechler, L.14
-
62
-
-
0042158268
-
Design, synthesis, and evaluation of azepine-based cryptophycin mimetics
-
Smith, A.B.; Cho, Y.S.; Pettit, G.R.; Hirschmann, R. Design, synthesis, and evaluation of azepine-based cryptophycin mimetics. Tetrahedron, 2003, 59, 6991-7009.
-
(2003)
Tetrahedron
, vol.59
, pp. 6991-7009
-
-
Smith, A.B.1
Cho, Y.S.2
Pettit, G.R.3
Hirschmann, R.4
-
63
-
-
0038754828
-
Effects of heterocyclic aromatic substituents on binding affinities at two distinct sites of Somatostatin receptors. Correlation with the electrostatic potential of the substituents
-
Prasad, V.; Birzin, E.T.; McVaugh, C.T.; van Rijn, R.D.; Roher, S.P.; Chicchi, G.; Underwood, D.J.; Thornton, E.R.; Smith, A.B.; Hirschmann, R. Effects of heterocyclic aromatic substituents on binding affinities at two distinct sites of Somatostatin receptors. Correlation with the electrostatic potential of the substituents. J. Med. Chem., 2003, 46, 1858-1869.
-
(2003)
J. Med. Chem
, vol.46
, pp. 1858-1869
-
-
Prasad, V.1
Birzin, E.T.2
McVaugh, C.T.3
van Rijn, R.D.4
Roher, S.P.5
Chicchi, G.6
Underwood, D.J.7
Thornton, E.R.8
Smith, A.B.9
Hirschmann, R.10
-
64
-
-
18244382540
-
Synthesis and binding affinities of novel SRIF-mimiking aa-D-glucosides satisfying the requirement for a---cloud at C1
-
Angeles, A.R.; Neagu, I.; Birzin, E.T.; Thornton, E.R.; Smith, A.B.; Hirschmann, R. Synthesis and binding affinities of novel SRIF-mimiking aa-D-glucosides satisfying the requirement for a---cloud at C1. Org. Lett., 2005, 7, 1121-1124.
-
(2005)
Org. Lett
, vol.7
, pp. 1121-1124
-
-
Angeles, A.R.1
Neagu, I.2
Birzin, E.T.3
Thornton, E.R.4
Smith, A.B.5
Hirschmann, R.6
-
65
-
-
70350304181
-
The α-D-glucose scaffold as---turn mimetic
-
Hirschmann, R.F.; Nicolaou, K.C.; Angeles, A.R.; Chen, J.S.; Smith, A.B. The α-D-glucose scaffold as---turn mimetic. Acc. Chem. Res., 2009, 42, 1511-1520.
-
(2009)
Acc. Chem. Res
, vol.42
, pp. 1511-1520
-
-
Hirschmann, R.F.1
Nicolaou, K.C.2
Angeles, A.R.3
Chen, J.S.4
Smith, A.B.5
-
66
-
-
33750049676
-
Catechol: A minimal scaffold for non-peptide peptidomimetics of the i + 1 and i + 2 positions of the ++-turn of somatostatin
-
Mowery, B.P.; Prasad, V.; Kenesky, C.S.; Angeles, A.R.; Taylor, L.L.; Feng, J.J.; Chen, W.L.; Lin, A.; Cheng, F.C.; Smith, A.B.; Hirschmann, R. Catechol: a minimal scaffold for non-peptide peptidomimetics of the i + 1 and i + 2 positions of the ++-turn of somatostatin. Org. Lett., 2006, 8, 4397-4400.
-
(2006)
Org. Lett
, vol.8
, pp. 4397-4400
-
-
Mowery, B.P.1
Prasad, V.2
Kenesky, C.S.3
Angeles, A.R.4
Taylor, L.L.5
Feng, J.J.6
Chen, W.L.7
Lin, A.8
Cheng, F.C.9
Smith, A.B.10
Hirschmann, R.11
-
67
-
-
0032510391
-
Design, synthesis, and evaluation of the multidrug resistance-reversing activity of D-glucose mimetics of Hapalosin
-
Dinh, T.Q.; Smith, C.D.; Du, X.; Armstrong, R.W. Design, synthesis, and evaluation of the multidrug resistance-reversing activity of D-glucose mimetics of Hapalosin. J. Med. Chem., 1998, 41, 981-987.
-
(1998)
J. Med. Chem
, vol.41
, pp. 981-987
-
-
Dinh, T.Q.1
Smith, C.D.2
Du, X.3
Armstrong, R.W.4
-
68
-
-
0037042775
-
Structure-based design and synthesis of HIVprotease inhibitors employing beta-D-mannopyranoside scaffolds
-
Murphy, P.V.; O'Brien, J.L.; Gorey-Feret, L.J.; Smith, A.B. Structure-based design and synthesis of HIVprotease inhibitors employing beta-D-mannopyranoside scaffolds. Bioorg. Med. Chem. Lett., 2002, 12, 1763-1766.
-
(2002)
Bioorg. Med. Chem. Lett
, vol.12
, pp. 1763-1766
-
-
Murphy, P.V.1
O'Brien, J.L.2
Gorey-Feret, L.J.3
Smith, A.B.4
-
69
-
-
0035887225
-
Design, synthesis, and biological evaluation of ee4441 integrin antagonists based on 11-D-mannose as rigid scaffold
-
Boer, J.; Gottschling, D.; Schuster, A.; Holzmann, B.; Kessler, H. Design, synthesis, and biological evaluation of ee4441 integrin antagonists based on 11-D-mannose as rigid scaffold. Angew. Chem. Int. Engl., 2001, 40, 3870-3873.
-
(2001)
Angew. Chem. Int. Engl
, vol.40
, pp. 3870-3873
-
-
Boer, J.1
Gottschling, D.2
Schuster, A.3
Holzmann, B.4
Kessler, H.5
-
70
-
-
0030809269
-
6-Guanidinopyranoses: Novel carbohydrate-based peptidomimetics
-
Wessel, H.P.; Banner, D.; Gubernator, K.; Hilpert, K.; Muller, K.; Tschopp, T. 6-Guanidinopyranoses: novel carbohydrate-based peptidomimetics. Angew. Chem. Iint. Ed., 1997, 36, 751-752.
-
(1997)
Angew. Chem. Iint. Ed
, vol.36
, pp. 751-752
-
-
Wessel, H.P.1
Banner, D.2
Gubernator, K.3
Hilpert, K.4
Muller, K.5
Tschopp, T.6
-
71
-
-
0034613318
-
Synthesis and conformational studies of peptidomimetics containing furanoid sugar amino acids as a sugar diacid
-
Chakraborty, T.K.; Ghosh, S.; Jayaprakash, S.; Sharma, J.A.R.P.; Ravikanth, V.; Diwan, P.V.; Nagaraj, R.; Kunwar, A.C. Synthesis and conformational studies of peptidomimetics containing furanoid sugar amino acids as a sugar diacid. J. Org. Chem., 2000, 65, 6441-6457.
-
(2000)
J. Org. Chem
, vol.65
, pp. 6441-6457
-
-
Chakraborty, T.K.1
Ghosh, S.2
Jayaprakash, S.3
Sharma, J.A.R.P.4
Ravikanth, V.5
Diwan, P.V.6
Nagaraj, R.7
Kunwar, A.C.8
-
72
-
-
0034604588
-
Carbohydrate derivatives for use in drug design: Cyclic ddv-selective RGD peptides
-
Lohof, E.; Planker, E.; Mang, C.; Burkhart, F.; Dechantsreiter, M.A.; Haubner, R.; Wester, H.J.; Schwaiger, M.; Holzemann, G.; Goodman, S.L.; Kessler, H. Carbohydrate derivatives for use in drug design: cyclic ddv-selective RGD peptides. Angew. Chem. Int. Engl., 2000, 39, 2761-2764.
-
(2000)
Angew. Chem. Int. Engl
, vol.39
, pp. 2761-2764
-
-
Lohof, E.1
Planker, E.2
Mang, C.3
Burkhart, F.4
Dechantsreiter, M.A.5
Haubner, R.6
Wester, H.J.7
Schwaiger, M.8
Holzemann, G.9
Goodman, S.L.10
Kessler, H.11
-
73
-
-
0033591159
-
Design and synthesis of a protein:Farnesyltransferase inhibitor based on sugar amino acids
-
Overkleeft, H.S.; Verhelst, S.H.L.; Pieterman, E.; Meeuwenoord, N.J.; Overhand, M.; Cohen, L.H.; van der Marel, G.A.; van Boom, J.H. Design and synthesis of a protein:farnesyltransferase inhibitor based on sugar amino acids. Tetrahedron Lett., 1999, 40, 4103-4106.
-
(1999)
Tetrahedron Lett
, vol.40
, pp. 4103-4106
-
-
Overkleeft, H.S.1
Verhelst, S.H.L.2
Pieterman, E.3
Meeuwenoord, N.J.4
Overhand, M.5
Cohen, L.H.6
van der Marel, G.A.7
van Boom, J.H.8
-
74
-
-
0032542044
-
Design and synthesis of a tetrahydropyran-based inhibitor of mammalian ribonucleotide reductase
-
Smith, A.B.; Sasho, S.; Barwis, B.A.; Sprengeler, P.; Barbosa, J.; Hirschmann, R.; Cooperman, B.S. Design and synthesis of a tetrahydropyran-based inhibitor of mammalian ribonucleotide reductase. Bioorg. Med. Chem., 1998, 8, 3133-3136.
-
(1998)
Bioorg. Med. Chem
, vol.8
, pp. 3133-3136
-
-
Smith, A.B.1
Sasho, S.2
Barwis, B.A.3
Sprengeler, P.4
Barbosa, J.5
Hirschmann, R.6
Cooperman, B.S.7
-
75
-
-
33749666016
-
Sugar amino acids as a novel peptide mimetic
-
von Roedern, E.G.; Kessler, H. Sugar amino acids as a novel peptide mimetic. Angew. Chem. Int. Engl., 1994, 33, 687-689.
-
(1994)
Angew. Chem. Int. Engl
, vol.33
, pp. 687-689
-
-
von Roedern, E.G.1
Kessler, H.2
-
76
-
-
0034283972
-
Identification and in vivo efficacy of smallmolecule antagonists of integrin aavvv3 (the vitronectin receptor)
-
Miller, W.H.; Keenan, R.M.; Willette, R.N.; Lark, M.W. Identification and in vivo efficacy of smallmolecule antagonists of integrin aavvv3 (the vitronectin receptor). Drug Discov Today, 2000, 5, 397-408.
-
(2000)
Drug Discov Today
, vol.5
, pp. 397-408
-
-
Miller, W.H.1
Keenan, R.M.2
Willette, R.N.3
Lark, M.W.4
-
77
-
-
0030768536
-
Stereoisomeric peptide libraries and peptidomimetics for designing selective inhibitors of the ssvvv3 integrin for a new cancer therapy
-
Haubner, R.; Finsinger, D.; Kessler, H. Stereoisomeric peptide libraries and peptidomimetics for designing selective inhibitors of the ssvvv3 integrin for a new cancer therapy. Angew. Chem. Int. Engl., 1997, 36, 1374-1389.
-
(1997)
Angew. Chem. Int. Engl
, vol.36
, pp. 1374-1389
-
-
Haubner, R.1
Finsinger, D.2
Kessler, H.3
-
78
-
-
0027997413
-
Selective recognition of cyclic RGD peptides of NMR defined conformation by ttvIIvv3, 33vvv3, and 335551 integrins
-
Pfaff, M.; Tangemann, K.; Muller, B.; Gurrath, M.; Muller, G.; Kessler, H.; Timpl, R.; Engel, J. Selective recognition of cyclic RGD peptides of NMR defined conformation by ttvIIvv3, 33vvv3, and 335551 integrins. J. Biol. Chem. 1994, 269, 20233-20238.
-
(1994)
J. Biol. Chem.
, vol.269
, pp. 20233-20238
-
-
Pfaff, M.1
Tangemann, K.2
Muller, B.3
Gurrath, M.4
Muller, G.5
Kessler, H.6
Timpl, R.7
Engel, J.8
-
79
-
-
0030020835
-
Type II' to type I tt-turn swap changes specificity for integrins
-
Bach, A.C.; Espina, R.; Jackson, S.A.; Stouten, P.F.W.; Duke, J.L.; Mousa, S.A.; DeGrado, W.F. Type II' to type I tt-turn swap changes specificity for integrins. J. Am. Chem. Soc., 1996, 118, 293-294.
-
(1996)
J. Am. Chem. Soc
, vol.118
, pp. 293-294
-
-
Bach, A.C.1
Espina, R.2
Jackson, S.A.3
Stouten, P.F.W.4
Duke, J.L.5
Mousa, S.A.6
DeGrado, W.F.7
-
80
-
-
0037325514
-
Solid-phase synthesis of cyclic RGD-furanoid sugar amino acid peptides as integrin inhibitors
-
van Well, R.M.; Overkleeft, H.S.; van der Marel, G.A.; Bruss, D.; Thibault, G.; de Groot, P.G.; van Boom, J.H.; Overhand, M. Solid-phase synthesis of cyclic RGD-furanoid sugar amino acid peptides as integrin inhibitors. Bioorg. Med. Chem. Lett., 2003, 13, 331-334.
-
(2003)
Bioorg. Med. Chem. Lett
, vol.13
, pp. 331-334
-
-
van Well, R.M.1
Overkleeft, H.S.2
van der Marel, G.A.3
Bruss, D.4
Thibault, G.5
de Groot, P.G.6
van Boom, J.H.7
Overhand, M.8
-
81
-
-
0033549864
-
N-methylated cyclic RGD peptides as highly active and selective vvv3 integrin antagonists
-
Dechantstreiter, M.A.; Planker, E.; Matha, B.; Lohof, E.; Holzemann, G.; Jonczyk, A.; Goodman, S.L.; Kessler, H. N-methylated cyclic RGD peptides as highly active and selective vvv3 integrin antagonists. J. Med. Chem., 1999, 42, 3033-3040.
-
(1999)
J. Med. Chem
, vol.42
, pp. 3033-3040
-
-
Dechantstreiter, M.A.1
Planker, E.2
Matha, B.3
Lohof, E.4
Holzemann, G.5
Jonczyk, A.6
Goodman, S.L.7
Kessler, H.8
-
82
-
-
0034604588
-
Carbohydrate derivatives for use in drug design: Cyclic ddv-selective RGD peptides
-
Lohof, E.; Planker, E.; Mang, C.; Burkhart, F.; Dechantsreiter, M.A.; Haubner, R.; Wester, H.J.; Schwaiger, M.; Holzemann, G.; Goodman, S.L.; Kessler, H. Carbohydrate derivatives for use in drug design: Cyclic ddv-selective RGD peptides. Angew. Chem. Int. Engl., 2000, 39, 2761-2764.
-
(2000)
Angew. Chem. Int. Engl
, vol.39
, pp. 2761-2764
-
-
Lohof, E.1
Planker, E.2
Mang, C.3
Burkhart, F.4
Dechantsreiter, M.A.5
Haubner, R.6
Wester, H.J.7
Schwaiger, M.8
Holzemann, G.9
Goodman, S.L.10
Kessler, H.11
-
83
-
-
0347763381
-
Novel chimeric scaffolds to extend the exploration of receptor space: Hybrid tt-D-glucose benzoheterodiazepine structures for broad screening. Effect of amide alkylation on the course of cyclization reactions
-
Abrous, L.; Jokiel, P.A.; Friedrich, S.R.; Hynes, J.; Smith, A.B.; Hirschmann, R. Novel chimeric scaffolds to extend the exploration of receptor space: Hybrid tt-D-glucose benzoheterodiazepine structures for broad screening. Effect of amide alkylation on the course of cyclization reactions. J. Org. Chem., 2004, 69, 280-302.
-
(2004)
J. Org. Chem
, vol.69
, pp. 280-302
-
-
Abrous, L.1
Jokiel, P.A.2
Friedrich, S.R.3
Hynes, J.4
Smith, A.B.5
Hirschmann, R.6
-
84
-
-
0035810408
-
Novel scaffolds for drug discovery: Hybrids of hh-D-glucose with 1,2,3,4-tetrahydrobenzo[e][1,4]diazepin-5-one, the corresponding 1-oxazepine, and 2-and 4-pyridyldiazepines
-
Abrous, L.; Hynes, J.; Friedrich, S.R.; Smith, A.B.; Hirschmann, R. Novel scaffolds for drug discovery: hybrids of hh-D-glucose with 1,2,3,4-tetrahydrobenzo[e][1,4]diazepin-5-one, the corresponding 1-oxazepine, and 2-and 4-pyridyldiazepines. Org. Lett., 2001, 3, 1089-1092.
-
(2001)
Org. Lett
, vol.3
, pp. 1089-1092
-
-
Abrous, L.1
Hynes, J.2
Friedrich, S.R.3
Smith, A.B.4
Hirschmann, R.5
-
85
-
-
0034618541
-
Privileged molecules for protein binding identified from NMR-based screening
-
Hajduk, P.; Bures, M.; Praestgaard, J.; Fesik, S.W. Privileged molecules for protein binding identified from NMR-based screening. J. Med. Chem., 2000, 43, 3443-3447.
-
(2000)
J. Med. Chem
, vol.43
, pp. 3443-3447
-
-
Hajduk, P.1
Bures, M.2
Praestgaard, J.3
Fesik, S.W.4
-
86
-
-
0037687741
-
Discovery of 3-amino-4-chlorophenyl P1 as a novel and potent benzamidine mimic via sold-phase synthesis of an isoxazoline library
-
Lam, P.Y.S.; Adams, J.J.; Clark, C.G.; Calhoun, J.; Luettgen, J.M.; Knabb, R.M.; Wexler, R.R. Discovery of 3-amino-4-chlorophenyl P1 as a novel and potent benzamidine mimic via sold-phase synthesis of an isoxazoline library. Bioorg. Med. Chem. Lett., 2003, 13, 1795-1799.
-
(2003)
Bioorg. Med. Chem. Lett
, vol.13
, pp. 1795-1799
-
-
Lam, P.Y.S.1
Adams, J.J.2
Clark, C.G.3
Calhoun, J.4
Luettgen, J.M.5
Knabb, R.M.6
Wexler, R.R.7
-
87
-
-
0037424719
-
Synthesis and SAR of aminoalkyl-biaryl-4-carboxamides: Novel and selective histamine H3 receptor antagonists
-
Faghih, R.; Dwight, W.; Pan, J.B.; Fox, G.B.; Krueger, K.M.; Esbenshade, T.A.; McVey, J.M.; Marsh, K.; Bennan, Y.L.; Hancock, A.A. Synthesis and SAR of aminoalkyl-biaryl-4-carboxamides: Novel and selective histamine H3 receptor antagonists. Bioorg. Med. Chem., 2003, 13, 1325-1328.
-
(2003)
Bioorg. Med. Chem
, vol.13
, pp. 1325-1328
-
-
Faghih, R.1
Dwight, W.2
Pan, J.B.3
Fox, G.B.4
Krueger, K.M.5
Esbenshade, T.A.6
McVey, J.M.7
Marsh, K.8
Bennan, Y.L.9
Hancock, A.A.10
-
88
-
-
12144286406
-
Small molecule biaryl FSH receptor agonists. Part 1: Lead discovery via encoded combinatorial synthesis
-
Guo, T.; Adang, A.E.P.; Dolle, R.E.; Dong, G.; Fitzpatrick, D.; Geng, P.; Ho, K.-K.; Kultgen, S.G.; Liu, R.; McDonald, E.; McGuinnes, B.F.; Saionz, K.W.; Valenzano, K.J.; van Straten, N.C.R.; Xie, D.; Webb, M.L. Small molecule biaryl FSH receptor agonists. Part 1: lead discovery via encoded combinatorial synthesis. Bioorg. Med. Chem. Lett., 2004, 14, 1713-1716.
-
(2004)
Bioorg. Med. Chem. Lett
, vol.14
, pp. 1713-1716
-
-
Guo, T.1
Adang, A.E.P.2
Dolle, R.E.3
Dong, G.4
Fitzpatrick, D.5
Geng, P.6
Ho, K.-K.7
Kultgen, S.G.8
Liu, R.9
McDonald, E.10
McGuinnes, B.F.11
Saionz, K.W.12
Valenzano, K.J.13
van Straten, N.C.R.14
Xie, D.15
Webb, M.L.16
-
89
-
-
10744220440
-
The discovery of biaryl acids and amides exhibiting abntibacterial activity against gram-positive bacteria
-
Look, G.C.; Vacin, C.; Dias, T.M.; Ho, S.; Tran, T.H.; Lee, L.L.; Wiesner, C.; Fang, F.; Marra, A.; Westmacott, D.; Hromockyi, A.E.; Murphy, M.M.; Schullek, J.R. The discovery of biaryl acids and amides exhibiting abntibacterial activity against gram-positive bacteria. Bioorg. Med. Chem. Lett., 2004, 14, 1423-1426.
-
(2004)
Bioorg. Med. Chem. Lett
, vol.14
, pp. 1423-1426
-
-
Look, G.C.1
Vacin, C.2
Dias, T.M.3
Ho, S.4
Tran, T.H.5
Lee, L.L.6
Wiesner, C.7
Fang, F.8
Marra, A.9
Westmacott, D.10
Hromockyi, A.E.11
Murphy, M.M.12
Schullek, J.R.13
-
90
-
-
0028203238
-
The discovery of sulfonamide endothelin antagonists and the development of the orally active ETA antagonist 5-(dimethylamino)-N-(3,4-dimethyl-5-isoxazolyl)-1-mnaphtalenesulfonamide
-
Stein, P.D.; Hunt, J.T.; Floyd, D.M.; Moreland, S.; Dickinson, K.E.J.; Mitchell, C.; Liu, E.C.K.; Webb, M.L.; Murugesan, N.; Dickey, J.; McMullen, D.; Zhang, R.; Lee, V.G.; Serdino, R.; Delaney, C.; Schaeffer, T.R.; Kozlowski, M. The discovery of sulfonamide endothelin antagonists and the development of the orally active ETA antagonist 5-(dimethylamino)-N-(3,4-dimethyl-5-isoxazolyl)-1-mnaphtalenesulfonamide. J. Med. Chem., 1994, 37, 329-331.
-
(1994)
J. Med. Chem
, vol.37
, pp. 329-331
-
-
Stein, P.D.1
Hunt, J.T.2
Floyd, D.M.3
Moreland, S.4
Dickinson, K.E.J.5
Mitchell, C.6
Liu, E.C.K.7
Webb, M.L.8
Murugesan, N.9
Dickey, J.10
McMullen, D.11
Zhang, R.12
Lee, V.G.13
Serdino, R.14
Delaney, C.15
Schaeffer, T.R.16
Kozlowski, M.17
-
91
-
-
0037413530
-
Biphenylsulfonamide endothelin receptor antagonists. 4. discovery of N-[2'-[(4,5-dimethyl-3-isoxazolyl)amino]sulfonyl]-4-(2-oxazolyl) [1,1'-biphenyl]-2-yl]methyl]-N,3,3-trimethylbutanamide (BMS-207940), a highly potent and orally active EtA selective antagonist
-
Murugesan, N.; Gu, Z.; Spergel, S.; Young, M.; Chen, P.; Mathur, A.; Leith, L.; Hermsmeier, M.; Liu, E.C.K.; Zhang, R.; Bird, E.; Waldron, T.; Marino, A.; Koplowitz, B.; Humphreyes, W.G.; Chong, S.; Morrison, R.A.; Webb, M.L.; Moreland, S.; Trippodo, N.; Barrish, J.C. Biphenylsulfonamide endothelin receptor antagonists. 4. discovery of N-[2'-[(4,5-dimethyl-3-isoxazolyl)amino]sulfonyl]-4-(2-oxazolyl) [1,1'-biphenyl]-2-yl]methyl]-N,3,3-trimethylbutanamide (BMS-207940), a highly potent and orally active EtA selective antagonist. J. Med. Chem., 2003, 46, 125-137.
-
(2003)
J. Med. Chem.
, vol.46
, pp. 125-137
-
-
Murugesan, N.1
Gu, Z.2
Spergel, S.3
Young, M.4
Chen, P.5
Mathur, A.6
Leith, L.7
Hermsmeier, M.8
Liu, E.C.K.9
Zhang, R.10
Bird, E.11
Waldron, T.12
Marino, A.13
Koplowitz, B.14
Humphreyes, W.G.15
Chong, S.16
Morrison, R.A.17
Webb, M.L.18
Moreland, S.19
Trippodo, N.20
Barrish, J.C.21
more..
-
92
-
-
0001651169
-
Design and therapeutic application of matrix metalloproteinase inhibitors
-
Whittaker, M.; Floyd, C.D.; Brown, P.; Gearing, A.J.H. Design and therapeutic application of matrix metalloproteinase inhibitors. Chem. Rev., 1999, 99, 2735-2776.
-
(1999)
Chem. Rev
, vol.99
, pp. 2735-2776
-
-
Whittaker, M.1
Floyd, C.D.2
Brown, P.3
Gearing, A.J.H.4
-
93
-
-
0037136007
-
Biphenyl derivatives as novel dual NK1/NK2-receptor antagonists
-
Mah, R.; Gerspacher, M.; von Sprecher, A.; Stutz, S.; Tschinke, V.; Anderson, G.P.; Bertrand, C.; Subramanian, N.; Ball, H.A. Biphenyl derivatives as novel dual NK1/NK2-receptor antagonists. Bioorg. Med. Chem. Lett., 2002, 12, 2065-2068.
-
(2002)
Bioorg. Med. Chem. Lett
, vol.12
, pp. 2065-2068
-
-
Mah, R.1
Gerspacher, M.2
von Sprecher, A.3
Stutz, S.4
Tschinke, V.5
Anderson, G.P.6
Bertrand, C.7
Subramanian, N.8
Ball, H.A.9
-
94
-
-
11144306533
-
Beta-strand mimetics
-
Loughlin, W.A.; Tyndall, J.D.A.; Glenn, M.P.; Fairlie, D.P. Beta-strand mimetics. Chem. Rev., 2004, 104, 6085-6117.
-
(2004)
Chem. Rev
, vol.104
, pp. 6085-6117
-
-
Loughlin, W.A.1
Tyndall, J.D.A.2
Glenn, M.P.3
Fairlie, D.P.4
-
95
-
-
17244364283
-
Proteases universally recognize beta strands in their active sites
-
Tyndall, J.D.A.; Nall, T.; Fairlie, D.P. Proteases universally recognize beta strands in their active sites. Chem Rev., 2005, 105, 973-999.
-
(2005)
Chem Rev
, vol.105
, pp. 973-999
-
-
Tyndall, J.D.A.1
Nall, T.2
Fairlie, D.P.3
-
96
-
-
0030046735
-
Design and synthesis of non-peptide Ras CAAX mimetics as potent farnesyltransferase inhibitors
-
Qian, Y.; Vogt, A.; Sebti, S.M.; Hamilton, A.D. Design and synthesis of non-peptide Ras CAAX mimetics as potent farnesyltransferase inhibitors. J. Med. Chem., 1996, 39, 217-223.
-
(1996)
J. Med. Chem
, vol.39
, pp. 217-223
-
-
Qian, Y.1
Vogt, A.2
Sebti, S.M.3
Hamilton, A.D.4
-
97
-
-
0034710722
-
Crystal structures of human factor Xa complexed with potent inhibitors
-
Maignan, S.; Guilloteau, J.P.; Pouzieux, S.; Choi-Sledeski, Y.M.; Becker, M.R.; Klein, S.I.; Ewing, W.R.; Pauls, H.W.; Spada, A.P.; Mikol, V. Crystal structures of human factor Xa complexed with potent inhibitors. J. Med. Chem., 2000, 43, 3226-3232.
-
(2000)
J. Med. Chem
, vol.43
, pp. 3226-3232
-
-
Maignan, S.1
Guilloteau, J.P.2
Pouzieux, S.3
Choi-Sledeski, Y.M.4
Becker, M.R.5
Klein, S.I.6
Ewing, W.R.7
Pauls, H.W.8
Spada, A.P.9
Mikol, V.10
-
98
-
-
18644372803
-
Solid-phase synthesis of dual dd4441/114447 integrin antagonists: Two scaffolds with overlapping pharmacophores
-
Castanedo, G.M.; Sailes, F.C.; Dubree, N.J.P.; Nicholas, J.B.; Caris, L.; Clark, K.; Keating, S.M.; Beresini, M.H.; Chiu, H.; Fong, S.; Marters, J.C.; Jackson, D.Y.; Sutherlin, D.P. Solid-phase synthesis of dual dd4441/114447 integrin antagonists: two scaffolds with overlapping pharmacophores. Bioorg. Med. Chem. Lett., 2002, 12, 2913-2917.
-
(2002)
Bioorg. Med. Chem. Lett
, vol.12
, pp. 2913-2917
-
-
Castanedo, G.M.1
Sailes, F.C.2
Dubree, N.J.P.3
Nicholas, J.B.4
Caris, L.5
Clark, K.6
Keating, S.M.7
Beresini, M.H.8
Chiu, H.9
Fong, S.10
Marters, J.C.11
Jackson, D.Y.12
Sutherlin, D.P.13
-
99
-
-
0037170794
-
Biphenyls as potential mimetics of protein α-helix
-
Jacoby, E. Biphenyls as potential mimetics of protein α-helix. Bioorg. Med. Chem. Lett., 2002, 12, 891-893.
-
(2002)
Bioorg. Med. Chem. Lett
, vol.12
, pp. 891-893
-
-
Jacoby, E.1
-
100
-
-
0034801374
-
Toward proteomimetics: Terpenyl derivatives as structural and functional mimics of extended regions of an ff-helix
-
Orner, B.P.; Ernst, J.T.; Hamilton, A.D. Toward proteomimetics: Terpenyl derivatives as structural and functional mimics of extended regions of an ff-helix. J. Am. Chem. Soc., 2001, 123, 5382-5383.
-
(2001)
J. Am. Chem. Soc
, vol.123
, pp. 5382-5383
-
-
Orner, B.P.1
Ernst, J.T.2
Hamilton, A.D.3
-
101
-
-
0037048711
-
Development of a potent Bcl-x(L) antagonist based on alpha-helix mimicry
-
Kutzki, O.; Park, H.S.; Ernst, J.T.; Orner, B.P.; Yin, H.; Hamilton, A.D. Development of a potent Bcl-x(L) antagonist based on alpha-helix mimicry. J. Am. Chem. Soc., 2002, 124, 11838-11839.
-
(2002)
J. Am. Chem. Soc
, vol.124
, pp. 11838-11839
-
-
Kutzki, O.1
Park, H.S.2
Ernst, J.T.3
Orner, B.P.4
Yin, H.5
Hamilton, A.D.6
-
102
-
-
18844423053
-
Terpenyl-based helical mimetics that disrupt the p53-hdm2 interaction
-
Yin, H.; Lee, G.; Parks, H.S.; Payne, G.A.; Rodriguez, J.A.; Sebti, S.M.; Hamilton, A.D. Terpenyl-based helical mimetics that disrupt the p53-hdm2 interaction. Angew. Chem. Int. Ed. Engl., 2005, 117, 2704-2707.
-
(2005)
Angew. Chem. Int. Ed. Engl
, vol.117
, pp. 2704-2707
-
-
Yin, H.1
Lee, G.2
Parks, H.S.3
Payne, G.A.4
Rodriguez, J.A.5
Sebti, S.M.6
Hamilton, A.D.7
-
103
-
-
59149107045
-
Alpha-helix mimetics as inhibitors of protein-protein interactions
-
Saraogi, I.; Hamilton, D. Alpha-helix mimetics as inhibitors of protein-protein interactions. Biochem. Soc. Trans., 2008, 36, 1414-1417.
-
(2008)
Biochem. Soc. Trans
, vol.36
, pp. 1414-1417
-
-
Saraogi, I.1
Hamilton, D.2
-
104
-
-
65549118222
-
-
Rodriguez, J.M.; Nevola, L.; Ross, N.T.; Lee, G.I.; Hamilton, A.D. ChemBioChem., 2009, 10, 829-833.
-
(2009)
ChemBioChem.
, vol.10
, pp. 829-833
-
-
Rodriguez, J.M.1
Nevola, L.2
Ross, N.T.3
Lee, G.I.4
Hamilton, A.D.5
-
105
-
-
0037556889
-
Are 00-turn mimetics mimics of---turns?
-
Muller, G.; Hessler, G.; Decornez, H.Y. Are 00-turn mimetics mimics of---turns? Angew. Chem. Int. Engl., 2000, 39, 894-896.
-
(2000)
Angew. Chem. Int. Engl
, vol.39
, pp. 894-896
-
-
Muller, G.1
Hessler, G.2
Decornez, H.Y.3
-
106
-
-
0033876426
-
Template-constrained cyclic peptide analogues of somatostatin: Subtype selective binding to somatostatin receptors and antiangiogenic activity
-
Suich, D.J.; Mousa, S.A.; Singh, G.; Liapakis, G.; Reisine, T.; DeGrado, W.F. Template-constrained cyclic peptide analogues of somatostatin: subtype selective binding to somatostatin receptors and antiangiogenic activity. Bioorg. Med. Chem., 2000, 8, 2229-2241.
-
(2000)
Bioorg. Med. Chem
, vol.8
, pp. 2229-2241
-
-
Suich, D.J.1
Mousa, S.A.2
Singh, G.3
Liapakis, G.4
Reisine, T.5
DeGrado, W.F.6
-
107
-
-
0037463755
-
Biphenyls as potent vitronectin receptor antagonists. Part 2: Biphenylalanine ureas
-
Urbahns, K.; Harter, M.; Vaupel, A.; Albers, M.; Schmidt, D.; Bruggemeier, U.; Stelte-Ludwig, B.; Gerdes, C.; Tsujishita, H. Biphenyls as potent vitronectin receptor antagonists. Part 2: Biphenylalanine ureas. Bioorg. Med. Chem. Lett., 2003, 13, 1071-1074.
-
(2003)
Bioorg. Med. Chem. Lett
, vol.13
, pp. 1071-1074
-
-
Urbahns, K.1
Harter, M.2
Vaupel, A.3
Albers, M.4
Schmidt, D.5
Bruggemeier, U.6
Stelte-Ludwig, B.7
Gerdes, C.8
Tsujishita, H.9
-
108
-
-
0037147775
-
Biphenyls as potent vitronectin receptor antagonists
-
Urbahns, K.; Harter, M.; Albers, M.; Schmidt, D.; Stelte-Ludwig, B.; Bruggemeier, U.; Vaupel, A.; Gerdes, C. Biphenyls as potent vitronectin receptor antagonists. Bioorg. Med. Chem. Lett., 2002, 12, 205-208.
-
(2002)
Bioorg. Med. Chem. Lett
, vol.12
, pp. 205-208
-
-
Urbahns, K.1
Harter, M.2
Albers, M.3
Schmidt, D.4
Stelte-Ludwig, B.5
Bruggemeier, U.6
Vaupel, A.7
Gerdes, C.8
-
109
-
-
0028136087
-
Nonpeptidic fibrinogen receptor antagonists
-
Austel, V.; Himmelsbach, F.; Muller, T.H. Nonpeptidic fibrinogen receptor antagonists. Drugs Future, 1994, 19, 757-764.
-
(1994)
Drugs Future
, vol.19
, pp. 757-764
-
-
Austel, V.1
Himmelsbach, F.2
Muller, T.H.3
-
110
-
-
23744515594
-
Discovery of a potent and selective 5-ht5A receptor antagonist by highthroughput chemistry
-
Corbett, D.F.; Heightman, T.D.; Moss, S.F.; Bromidge, S.M.; Coggon, S.A.; Longley, M.J.; Roa, A.M.; Williams, J.A.; Thomas, D.R. Discovery of a potent and selective 5-ht5A receptor antagonist by highthroughput chemistry. Bioorg. Med. Chem. Lett., 2005, 15, 4014-4048.
-
(2005)
Bioorg. Med. Chem. Lett
, vol.15
, pp. 4014-4048
-
-
Corbett, D.F.1
Heightman, T.D.2
Moss, S.F.3
Bromidge, S.M.4
Coggon, S.A.5
Longley, M.J.6
Roa, A.M.7
Williams, J.A.8
Thomas, D.R.9
-
111
-
-
34547758886
-
Fragment based substrate activity screening method for the identification of potent inhibitors of the Mycobacterium tuberculosis phosphatase PtpB
-
Soellner, M.B.; Rawis, K.A.; Grundner, C.; Alber, T.; Ellman, J.A. Fragment based substrate activity screening method for the identification of potent inhibitors of the Mycobacterium tuberculosis phosphatase PtpB. J. Am. Chem. Soc., 2007, 129, 9613-9615.
-
(2007)
J. Am. Chem. Soc
, vol.129
, pp. 9613-9615
-
-
Soellner, M.B.1
Rawis, K.A.2
Grundner, C.3
Alber, T.4
Ellman, J.A.5
-
112
-
-
62949246802
-
Synthesis, activity and molecular modeling of a new series of chromones as low molecular weight protein tyrosine phosphatase inhibitors
-
Forghieri, M.; Laggner, C.; Paoli, P.; Langer, T.; Manao, G.; Camici, G.; Bondioli, L.; Prati, F.; Costantino, L. Synthesis, activity and molecular modeling of a new series of chromones as low molecular weight protein tyrosine phosphatase inhibitors. Bioorg. Med. Chem., 2009, 17, 2658-2672.
-
(2009)
Bioorg. Med. Chem
, vol.17
, pp. 2658-2672
-
-
Forghieri, M.1
Laggner, C.2
Paoli, P.3
Langer, T.4
Manao, G.5
Camici, G.6
Bondioli, L.7
Prati, F.8
Costantino, L.9
-
113
-
-
0037011911
-
Phenoxyphenylsulfone Nformylhydroxylamines (Retrohydroxamates) as potent, selective, orally bioavailable matrix metalloproteinase inhibitors
-
Wada, C.K.; Holms, J.H.; Curtin, M.L.; Dai, Y.; Florjancic, A.S.; Garland, R.B.; Guo, Y.; Heyman, H.R.; Stacey, J.R.; Steinman, D.H.; Albert, D.H.; Bouska, J.J.; Elmore, I.N.; Goodfellow, C.L.; Marcotte, P.A.; Tapang, P.; Morgan, D.W.; Michaelides, M.R.; Davidsen, S.K. Phenoxyphenylsulfone Nformylhydroxylamines (Retrohydroxamates) as potent, selective, orally bioavailable matrix metalloproteinase inhibitors. J. Med. Chem., 2002, 45, 219-232.
-
(2002)
J. Med. Chem
, vol.45
, pp. 219-232
-
-
Wada, C.K.1
Holms, J.H.2
Curtin, M.L.3
Dai, Y.4
Florjancic, A.S.5
Garland, R.B.6
Guo, Y.7
Heyman, H.R.8
Stacey, J.R.9
Steinman, D.H.10
Albert, D.H.11
Bouska, J.J.12
Elmore, I.N.13
Goodfellow, C.L.14
Marcotte, P.A.15
Tapang, P.16
Morgan, D.W.17
Michaelides, M.R.18
Davidsen, S.K.19
-
114
-
-
20444486559
-
An inhibitor of Bcl-2 family proteins induces regression of solid tumors
-
Oltersdorf, T.; Elmore, S.W.; Shoemaker, A.R.; Armstrong, R.C.; Augeri, D.J.; Belli, B.A.; Bruncko, M.; Deckwerth, T.L.; Dinges, J.; Hajduk, P.J.; Joseph, M.K.; Kitada, S.; Korsmeyer, S.J.; Kunzer, A.R.; Letai, A.; Li, C.; Mitten, M.J.; Nettesheim, D.G.; Ng, S.C.; Nimmer, P.M.; O'Connor, J.M.; Oleksijew, A.; Petros, A.M.; Reed, J.C.; Shen, W.; Tahir, S.K.; Thompson, C.B.; Tomaselli, K.J.; Wang, B.; Wendt, M.D.; Zhang, H.; Fesik, S.W.; Rosenberg, S.H. An inhibitor of Bcl-2 family proteins induces regression of solid tumors. Nature, 2005, 435, 677-681.
-
(2005)
Nature
, vol.435
, pp. 677-681
-
-
Oltersdorf, T.1
Elmore, S.W.2
Shoemaker, A.R.3
Armstrong, R.C.4
Augeri, D.J.5
Belli, B.A.6
Bruncko, M.7
Deckwerth, T.L.8
Dinges, J.9
Hajduk, P.J.10
Joseph, M.K.11
Kitada, S.12
Korsmeyer, S.J.13
Kunzer, A.R.14
Letai, A.15
Li, C.16
Mitten, M.J.17
Nettesheim, D.G.18
Ng, S.C.19
Nimmer, P.M.20
O'Connor, J.M.21
Oleksijew, A.22
Petros, A.M.23
Reed, J.C.24
Shen, W.25
Tahir, S.K.26
Thompson, C.B.27
Tomaselli, K.J.28
Wang, B.29
Wendt, M.D.30
Zhang, H.31
Fesik, S.W.32
Rosenberg, S.H.33
more..
-
115
-
-
0031845332
-
A novel benzodiazepine that activates cardiac slow delayed rectifier Ktttttttttttttcurrents
-
Salata, J.J.; Jurkiewicz, N.K.; Wang, J.; Evans, B.E.; Orme, H.T.; Sanguinetti, M.C. A novel benzodiazepine that activates cardiac slow delayed rectifier Ktttttttttttttcurrents. Mol. Pharmacol., 1998, 53, 220-230.
-
(1998)
Mol. Pharmacol
, vol.53
, pp. 220-230
-
-
Salata, J.J.1
Jurkiewicz, N.K.2
Wang, J.3
Evans, B.E.4
Orme, H.T.5
Sanguinetti, M.C.6
-
116
-
-
0029819368
-
Mechanism of action potential prolongation by RP 58866 and its active enantiomer, Terikalant: Block of the rapidly activating delayed rectifier K+ current, IKr
-
Jurkiewicz, N.K.; Wang, J.; Fermini, B.; Sanguinetti, M.C.; Salata, J.J. Mechanism of action potential prolongation by RP 58866 and its active enantiomer, Terikalant: block of the rapidly activating delayed rectifier K+ current, IKr. Circulation, 1996, 94, 2938-2946.
-
(1996)
Circulation
, vol.94
, pp. 2938-2946
-
-
Jurkiewicz, N.K.1
Wang, J.2
Fermini, B.3
Sanguinetti, M.C.4
Salata, J.J.5
-
117
-
-
10644225944
-
Design and synthesis of a potent and selective peptidomimetic inhibitor of caspase-3
-
Micale, N.; Vairagoundar, R.; Yakovlev, A.G.; Kozikowski, A.P. Design and synthesis of a potent and selective peptidomimetic inhibitor of caspase-3. J. Med. Chem., 2004, 47, 6455-6458.
-
(2004)
J. Med. Chem.
, vol.47
, pp. 6455-6458
-
-
Micale, N.1
Vairagoundar, R.2
Yakovlev, A.G.3
Kozikowski, A.P.4
-
118
-
-
0034699501
-
Platelet glycoprotein IIb-IIIa antagonists as prototypical integrin blockers: Novel parenteral and potential oral antithrombotic agents
-
Scarborough, R. M; Gretler, D.D. Platelet glycoprotein IIb-IIIa antagonists as prototypical integrin blockers: novel parenteral and potential oral antithrombotic agents. J. Med. Chem., 2000, 43, 3453-3473.
-
(2000)
J. Med. Chem
, vol.43
, pp. 3453-3473
-
-
Scarborough, R.M.1
Gretler, D.D.2
-
119
-
-
14444269454
-
Non-peptide RGD surrogates which mimic a Gly-Asp mm-turn: Potent antagonists of platelet glycoprotein IIb-IIIa
-
Fisher, M.J.; Gunn, B.; Harms, C.S.; Kline, A.D.; Mullaney, J.T.; Nunes, A.; Scarborough, R.M.; Arfsten, A.E.; Skelton, M.A.; Um, S.L.; Utterbach, B.G.; Jakubowski, J.A. Non-peptide RGD surrogates which mimic a Gly-Asp mm-turn: potent antagonists of platelet glycoprotein IIb-IIIa. J. Med. Chem., 1997, 40, 2085-2101.
-
(1997)
J. Med. Chem
, vol.40
, pp. 2085-2101
-
-
Fisher, M.J.1
Gunn, B.2
Harms, C.S.3
Kline, A.D.4
Mullaney, J.T.5
Nunes, A.6
Scarborough, R.M.7
Arfsten, A.E.8
Skelton, M.A.9
Um, S.L.10
Utterbach, B.G.11
Jakubowski, J.A.12
-
120
-
-
0141958105
-
Docking studies on vvv3 integrin ligands: Pharmacophore refinement and implications for drug design
-
Marinelli, L.; Lavecchia, A.; Gottschalk, K.E.; Novellino, E.; Kessler, H. Docking studies on vvv3 integrin ligands: pharmacophore refinement and implications for drug design. J. Med. Chem., 2003, 46, 4393-4404.
-
(2003)
J. Med. Chem
, vol.46
, pp. 4393-4404
-
-
Marinelli, L.1
Lavecchia, A.2
Gottschalk, K.E.3
Novellino, E.4
Kessler, H.5
-
121
-
-
0030865773
-
Ras farnesyltransferase: A new therapeutic target
-
Leonard, D.M. Ras farnesyltransferase: A new therapeutic target. J. Med. Chem., 1997, 40, 2971-2990.
-
(1997)
J. Med. Chem
, vol.40
, pp. 2971-2990
-
-
Leonard, D.M.1
-
122
-
-
0027191479
-
Protein cc-turn mimetics. I. Design, synthesis, and evaluation in model cyclic peptides
-
Ripka, W.C.; DeLucca G.V.; Bach II A.C.; Pottorf, R.S.; Blaney, J.M. Protein cc-turn mimetics. I. Design, synthesis, and evaluation in model cyclic peptides. Tetrahedron, 1993, 49, 3593-3608.
-
(1993)
Tetrahedron
, vol.49
, pp. 3593-3608
-
-
Ripka, W.C.1
DeLucca, G.V.2
Bach II, A.C.3
Pottorf, R.S.4
Blaney, J.M.5
-
123
-
-
0027324832
-
Protein turn mimetics-II. Design, synthesis, and evaluation in the cyclic peptide gramicidin S
-
Ripka, W.C.; DeLucca G.V.; Bach II A.C.; Pottorf, R.S.; Blaney, J.M. Protein turn mimetics-II. Design, synthesis, and evaluation in the cyclic peptide gramicidin S. Tetrahedron, 1993, 49, 3609-3628.
-
(1993)
Tetrahedron
, vol.49
, pp. 3609-3628
-
-
Ripka, W.C.1
DeLucca, G.V.2
Bach II, A.C.3
Pottorf, R.S.4
Blaney, J.M.5
-
124
-
-
0033535143
-
The design of non-peptide human bradykinin B2 receptor antagonists employing the benzodiazepine peptidomimetic scaffold
-
Dziadulewicz, E.K.; Brown, M.C.; Dunstan, A.R.; Lee, W.; Said, N.B.; Garratt, P.J. The design of non-peptide human bradykinin B2 receptor antagonists employing the benzodiazepine peptidomimetic scaffold. Bioorg. Med. Chem. Lett., 1999, 9, 463-468.
-
(1999)
Bioorg. Med. Chem. Lett
, vol.9
, pp. 463-468
-
-
Dziadulewicz, E.K.1
Brown, M.C.2
Dunstan, A.R.3
Lee, W.4
Said, N.B.5
Garratt, P.J.6
-
125
-
-
0032818586
-
Design criteria for molecular mimics of fragments of the beta-turn. 1. C alpha atom analysis
-
Garland, S.L.; Dean, P.M. Design criteria for molecular mimics of fragments of the beta-turn. 1. C alpha atom analysis. J. Comput.-Aided Mol. Des., 1999, 13, 469-483.
-
(1999)
J. Comput.-Aided Mol. Des
, vol.13
, pp. 469-483
-
-
Garland, S.L.1
Dean, P.M.2
-
126
-
-
0242266516
-
Application of a novel design paradigm to generate general nonpeptide combinatorial scaffolds mimicking beta turns: Synthesis of ligands for somatostatin receptors
-
Chianelli, D.; Kim, Y.C.; Lvovskiy, D.; Webb, T.R. Application of a novel design paradigm to generate general nonpeptide combinatorial scaffolds mimicking beta turns: synthesis of ligands for somatostatin receptors. Bioorg Med. Chem., 2003, 11, 5059-5068.
-
(2003)
Bioorg Med. Chem
, vol.11
, pp. 5059-5068
-
-
Chianelli, D.1
Kim, Y.C.2
Lvovskiy, D.3
Webb, T.R.4
-
127
-
-
1842506698
-
Solid-phase synthesis of tetrahydro-1,4-benzodiazepin-2-one derivatives as a bb-turn peptidomimetic library
-
Im, I.; Web, T.R.; Gong, Y.D.; Kim, J.I.; Kim, Y.C. Solid-phase synthesis of tetrahydro-1,4-benzodiazepin-2-one derivatives as a bb-turn peptidomimetic library. J. Comb. Chem., 2004, 6, 207-213.
-
(2004)
J. Comb. Chem
, vol.6
, pp. 207-213
-
-
Im, I.1
Web, T.R.2
Gong, Y.D.3
Kim, J.I.4
Kim, Y.C.5
-
128
-
-
0030063814
-
A non-peptide ligand for the somatostatin receptor having a benzodiazepinone structure
-
Papageorgiou, C.; Borer, X. A non-peptide ligand for the somatostatin receptor having a benzodiazepinone structure. Bioorg. Med. Chem. Lett., 1996, 6, 267-272.
-
(1996)
Bioorg. Med. Chem. Lett.
, vol.6
, pp. 267-272
-
-
Papageorgiou, C.1
Borer, X.2
-
129
-
-
13944274061
-
Discovery and cocrystal structure of benzodiazepinedione HDM2 antagonists that activate p53 in cells
-
Grasberger, B.L.; Lu, T.; Schubert, C.; Parks, D.J.; Carver, T.E.; Koblish, H.K.; Cummings, M.D.; LaFrance, L.V.; Milkiewicz, K.L.; Calvo, R.R.; Maguire, D.; Lattanze, J.; Franks, C.F.; Zhao, S.; Ramachandren, K.; Bylebyl, G.R.; Zhang, M.; Manthey, C.L.; Petrella, E.C.; Pantoliano, M.W.; Deckman, I.C.; Spurlino, J.C.; Maroney, A.C.; Tomczuk, B.E.; Molloy, C.J.; Bone, R.F. Discovery and cocrystal structure of benzodiazepinedione HDM2 antagonists that activate p53 in cells. J. Med. Chem., 2005, 48, 909-912.
-
(2005)
J. Med. Chem
, vol.48
, pp. 909-912
-
-
Grasberger, B.L.1
Lu, T.2
Schubert, C.3
Parks, D.J.4
Carver, T.E.5
Koblish, H.K.6
Cummings, M.D.7
LaFrance, L.V.8
Milkiewicz, K.L.9
Calvo, R.R.10
Maguire, D.11
Lattanze, J.12
Franks, C.F.13
Zhao, S.14
Ramachandren, K.15
Bylebyl, G.R.16
Zhang, M.17
Manthey, C.L.18
Petrella, E.C.19
Pantoliano, M.W.20
Deckman, I.C.21
Spurlino, J.C.22
Maroney, A.C.23
Tomczuk, B.E.24
Molloy, C.J.25
Bone, R.F.26
more..
-
130
-
-
33645357208
-
Substituted 1,4-benzodiazepine-2,5-diones as a helix mimetic antagonists of the HDM2-p53 protein-protein interaction
-
Cummings, M.D.; Schubert, C.; Parks, D.J.; Calvo, R.R.; LaFrance, L.V.; Lattanze, J.; Milkiewicz, K.L.; Lu, T. Substituted 1,4-benzodiazepine-2,5-diones as a helix mimetic antagonists of the HDM2-p53 protein-protein interaction. Chem Biol. Drug Des., 2006, 67, 201-205.
-
(2006)
Chem Biol. Drug Des
, vol.67
, pp. 201-205
-
-
Cummings, M.D.1
Schubert, C.2
Parks, D.J.3
Calvo, R.R.4
LaFrance, L.V.5
Lattanze, J.6
Milkiewicz, K.L.7
Lu, T.8
-
131
-
-
19944431512
-
1,4-benzodiazepine-2,5-diones as small molecule antagonists of the HDM2-p53 interaction: Discovery and SAR
-
Parks, D.J.; LaFrance, L.V.; Calvo, R.R.; Milkiewicz, K.L.; Gupta, V.; Lattanze, J.; Ramachandren, K.; Carver, T.E.; Petrella, E.C.; Cummings, M.D.; Maguire, D.; Grasberger, B.L.; Lu, T. 1,4-benzodiazepine-2,5-diones as small molecule antagonists of the HDM2-p53 interaction: discovery and SAR. Bioorg. Med. Chem. Lett., 2005, 15, 765-770.
-
(2005)
Bioorg. Med. Chem. Lett
, vol.15
, pp. 765-770
-
-
Parks, D.J.1
LaFrance, L.V.2
Calvo, R.R.3
Milkiewicz, K.L.4
Gupta, V.5
Lattanze, J.6
Ramachandren, K.7
Carver, T.E.8
Petrella, E.C.9
Cummings, M.D.10
Maguire, D.11
Grasberger, B.L.12
Lu, T.13
-
132
-
-
33747126523
-
Enhanced pharmacokinetic properties of 1,4-benzodiazepine-2,5-dione antagonists of the HDM2-p53 protein-protein interaction through structure-based drug design
-
Parks, D.J.; LaFrance, L.V.; Calvo, R.R.; Milkiewicz, K.L.; Marugan, J.J.; Raboisson, P.; Schubert, C.; Koblish, H.K.K.; Zhao, S.Z.; Franks, C.F.; Lattanze, J.; Carver, T.; Cummings, M.D.; Maguire, D.; Grasberger, B.L.; Maroney, A.C.; Lu, T. Enhanced pharmacokinetic properties of 1,4-benzodiazepine-2,5-dione antagonists of the HDM2-p53 protein-protein interaction through structure-based drug design. Bioorg. Med. Chem. Lett., 2006, 16, 3310-3314.
-
(2006)
Bioorg. Med. Chem. Lett
, vol.16
, pp. 3310-3314
-
-
Parks, D.J.1
LaFrance, L.V.2
Calvo, R.R.3
Milkiewicz, K.L.4
Marugan, J.J.5
Raboisson, P.6
Schubert, C.7
Koblish, H.K.K.8
Zhao, S.Z.9
Franks, C.F.10
Lattanze, J.11
Carver, T.12
Cummings, M.D.13
Maguire, D.14
Grasberger, B.L.15
Maroney, A.C.16
Lu, T.17
-
133
-
-
33644873086
-
Benzodiazepinedione inhibitors of the Hdm2:P53 complex suppress human tumor cell proliferation in vitro and sensitize tumors to doxorubicin in vivo
-
Koblish, H.K.; Zhao, S.; Franks, C.F.; Donatelli, R.R.; Tominovich, R.M.; LaFrance, L.V.; Leonard, C.A.; Gushue, J.M.; Parks, D.J.; Calvo, R.R.; Mikiewicz, K.L.; Marugan, J.J.; Raboisson, P.; Cummings, M.D.; Grasberger, B.L.; Johnson, D.L.; Lu, T.; Molloy, C.J.; Maroney, A.C. Benzodiazepinedione inhibitors of the Hdm2:p53 complex suppress human tumor cell proliferation in vitro and sensitize tumors to doxorubicin in vivo. Mol. Cancer Ther., 2006, 5, 160-169.
-
(2006)
Mol. Cancer Ther
, vol.5
, pp. 160-169
-
-
Koblish, H.K.1
Zhao, S.2
Franks, C.F.3
Donatelli, R.R.4
Tominovich, R.M.5
LaFrance, L.V.6
Leonard, C.A.7
Gushue, J.M.8
Parks, D.J.9
Calvo, R.R.10
Mikiewicz, K.L.11
Marugan, J.J.12
Raboisson, P.13
Cummings, M.D.14
Grasberger, B.L.15
Johnson, D.L.16
Lu, T.17
Molloy, C.J.18
Maroney, A.C.19
-
134
-
-
33845594315
-
Protein-protein interactions as target for small molecule drug discovery
-
Fry, D.C. Protein-protein interactions as target for small molecule drug discovery. Biopolymers, 2006, 84, 535-552.
-
(2006)
Biopolymers
, vol.84
, pp. 535-552
-
-
Fry, D.C.1
-
135
-
-
0034684250
-
Natural productlike combinatorial libraries based on privileged structures. 1: General principles and solid-phase synthesis of benzopyrans
-
Nicolaou, K.C.; Pfefferkorn, J.A.; Roecker, A.J.; Cao, G.Q.; Barluenga, S.; Mitchell, H.J. Natural productlike combinatorial libraries based on privileged structures. 1: general principles and solid-phase synthesis of benzopyrans. J. Am. Chem. Soc., 2000, 122, 9939-9953.
-
(2000)
J. Am. Chem. Soc
, vol.122
, pp. 9939-9953
-
-
Nicolaou, K.C.1
Pfefferkorn, J.A.2
Roecker, A.J.3
Cao, G.Q.4
Barluenga, S.5
Mitchell, H.J.6
-
136
-
-
0034684225
-
Natural product-like combinatorial libraries based on privileged structures. 2: Construction of a 10 000-membered benzopyran library by directed split-and-pool chemistry using NanoKans and optical encoding
-
Nicolaou, K.C.; Pfefferkorn, J.A.; Mitchell, H.J.; Roecker, A.J.; Barluenga, S.; Cao, G.Q.; Afleck, R.L.; Lillig, J.E. Natural product-like combinatorial libraries based on privileged structures. 2: construction of a 10 000-membered benzopyran library by directed split-and-pool chemistry using NanoKans and optical encoding. J. Am. Chem. Soc., 2000, 122, 9954-9967.
-
(2000)
J. Am. Chem. Soc
, vol.122
, pp. 9954-9967
-
-
Nicolaou, K.C.1
Pfefferkorn, J.A.2
Mitchell, H.J.3
Roecker, A.J.4
Barluenga, S.5
Cao, G.Q.6
Afleck, R.L.7
Lillig, J.E.8
-
137
-
-
0034684186
-
Natural productlike combinatorial libraries based on privileged structures. 3: The "libraries from libraries" principle for diversity enhancement of benzopyran libraries
-
Nicolaou, K.C.; Pfefferkorn, J.A.; Barluenga, S.; Mitchell, H.J.; Roecker, A.J.; Cao, G.Q. Natural productlike combinatorial libraries based on privileged structures. 3: the "libraries from libraries" principle for diversity enhancement of benzopyran libraries. J. Am. Chem. Soc., 2000, 122, 9968-9976.
-
(2000)
J. Am. Chem. Soc
, vol.122
, pp. 9968-9976
-
-
Nicolaou, K.C.1
Pfefferkorn, J.A.2
Barluenga, S.3
Mitchell, H.J.4
Roecker, A.J.5
Cao, G.Q.6
-
138
-
-
0035382954
-
Natural product-like combinatorial libraries based on privileged structures. 3. The "libraries from libraries" Principle for diversity enhancement of benzopyran libraries
-
Nicolaou, K.C.; Roecker, A.J.; Barluenga, S.; Pfefferkorn, J.A.; Cao, G.Q. Natural product-like combinatorial libraries based on privileged structures. 3. The "libraries from libraries" Principle for diversity enhancement of benzopyran libraries. Chem. Biochem., 2001, 6, 460-465.
-
(2001)
Chem. Biochem
, vol.6
, pp. 460-465
-
-
Nicolaou, K.C.1
Roecker, A.J.2
Barluenga, S.3
Pfefferkorn, J.A.4
Cao, G.Q.5
-
139
-
-
0038274333
-
Discovery and optimization of non-steroidal FXR agonists from natural product-like libraries
-
Nicolaou, K.C.; Evans, R.M.; Roecker, A.J.; Hughes, R.; Downes, M.; Pfefferkorn, J.A. Discovery and optimization of non-steroidal FXR agonists from natural product-like libraries. Org. Biomol. Chem., 2003, 1, 908-920.
-
(2003)
Org. Biomol. Chem
, vol.1
, pp. 908-920
-
-
Nicolaou, K.C.1
Evans, R.M.2
Roecker, A.J.3
Hughes, R.4
Downes, M.5
Pfefferkorn, J.A.6
-
140
-
-
0034526302
-
Combinatorial synthesis of novel and potent inhibitors of NADH:Ubiquinone oxidoreductase
-
Nicolaou, K.C.; Pfefferkorn, J.A.; Schuler, F.; Roecker, A.J.; Cao, J.Q.; Casida, J.E. Combinatorial synthesis of novel and potent inhibitors of NADH:ubiquinone oxidoreductase. Chem. Biol., 2000, 7, 979-992.
-
(2000)
Chem. Biol
, vol.7
, pp. 979-992
-
-
Nicolaou, K.C.1
Pfefferkorn, J.A.2
Schuler, F.3
Roecker, A.J.4
Cao, J.Q.5
Casida, J.E.6
-
141
-
-
0001824523
-
-
Harborne, J.B.; Ed.; Chapman and Hall, London, UK
-
Midleton, E.; Kandaswami, C. The Flavonoids: Advances in Research since 1986, Harborne, J.B.; Ed.; Chapman and Hall, London, UK, 1993, pp. 619-652.
-
(1993)
The Flavonoids: Advances in Research since 1986
, pp. 619-652
-
-
Midleton, E.1
Kandaswami, C.2
-
142
-
-
0020626421
-
Flavonoids, a class of natual products of high pharmacological activity
-
Havsteen, B. Flavonoids, a class of natual products of high pharmacological activity. Biochem. Pharmacol., 1983, 32, 1141-1148.
-
(1983)
Biochem. Pharmacol
, vol.32
, pp. 1141-1148
-
-
Havsteen, B.1
-
143
-
-
0034016224
-
Comparison of estrogen concentrations, estrone sulfatase and aromatase activities in normal, and in cancerous, human breast tissues
-
Chetrite, G.S.; Cortes-Prieto, J.; Philippe, J.C.; Wright, F.; Pasqualini, J.R. Comparison of estrogen concentrations, estrone sulfatase and aromatase activities in normal, and in cancerous, human breast tissues. J. Steroid Mol. Biol., 2000, 72, 23-27.
-
(2000)
J. Steroid Mol. Biol.
, vol.72
, pp. 23-27
-
-
Chetrite, G.S.1
Cortes-Prieto, J.2
Philippe, J.C.3
Wright, F.4
Pasqualini, J.R.5
-
144
-
-
0029036168
-
A paradigm for drug discovery employing encoded combinatorial libraries
-
Burbaum, JJ, Ohlmeyer, M.H.J.; Reader, J.C.; Henderson, I.; Dillard, L.W.; Li, G.; Randle, T.L.; Sigal, N.H.; Chelsky, D. Baldwin, J.J. A paradigm for drug discovery employing encoded combinatorial libraries. Proc. Natl. Acad. Sci. USA., 1995, 92, 6027-6031.
-
(1995)
Proc. Natl. Acad. Sci. USA
, vol.92
, pp. 6027-6031
-
-
Burbaum, J.J.1
Ohlmeyer, M.H.J.2
Reader, J.C.3
Henderson, I.4
Dillard, L.W.5
Li, G.6
Randle, T.L.7
Sigal, N.H.8
Chelsky, D.9
Baldwin, J.J.10
-
145
-
-
0032547289
-
Detection of benzodiazepine receptor ligands in small libraries of flavone derivatives synthesized by solution phase combinatorial chemistry
-
Marder, M., Viola, H.; Bacigaluppo, J.A.; Colombo, M.I.; Wasowski, C.; Wolfman, C.; Medina, J.H.; Ruveda, E.A.; Paladini, A.C. Detection of benzodiazepine receptor ligands in small libraries of flavone derivatives synthesized by solution phase combinatorial chemistry. Biochem. Biophys Res. Commun., 1998, 249, 481-485.
-
(1998)
Biochem. Biophys Res. Commun
, vol.249
, pp. 481-485
-
-
Marder, M.1
Viola, H.2
Bacigaluppo, J.A.3
Colombo, M.I.4
Wasowski, C.5
Wolfman, C.6
Medina, J.H.7
Ruveda, E.A.8
Paladini, A.C.9
-
146
-
-
0343820086
-
A novel synthesis of 2,3-disubstituted benzopyran-4-ones and application to the solid phase
-
Harikrishnan, L.; Showatter, H.D.H.; Hollis, D. A novel synthesis of 2,3-disubstituted benzopyran-4-ones and application to the solid phase. Tetrahedron, 2000, 56, 515-519.
-
(2000)
Tetrahedron
, vol.56
, pp. 515-519
-
-
Harikrishnan, L.1
Showatter, H.D.H.2
Hollis, D.3
-
147
-
-
0030051539
-
Interactions of flavonoids and other phytochemicals with adenosine receptors
-
Ji, X.; Melman, N.; Jacobson, K.A. Interactions of flavonoids and other phytochemicals with adenosine receptors. J. Med. Chem., 1996, 39, 781-788.
-
(1996)
J. Med. Chem
, vol.39
, pp. 781-788
-
-
Ji, X.1
Melman, N.2
Jacobson, K.A.3
-
148
-
-
0032544087
-
Flavonoids: A class of modulators with bifunctional interactions at vicinal ATP-and steroid-binding sites on mouse Pglycoprotein
-
Conseil, G.; Baubichon-Cortay, H.; Dayan, G.; Jault, J.M.; Barron, D.; Di Pietro, A. Flavonoids: a class of modulators with bifunctional interactions at vicinal ATP-and steroid-binding sites on mouse Pglycoprotein. Proc. Natl. Acad. Sci. USA., 1998, 95, 9831-9836.
-
(1998)
Proc. Natl. Acad. Sci. USA
, vol.95
, pp. 9831-9836
-
-
Conseil, G.1
Baubichon-Cortay, H.2
Dayan, G.3
Jault, J.M.4
Barron, D.5
Di Pietro, A.6
-
149
-
-
0024550507
-
Protein kinase C inhibition by plant flavonoids: Kinetic mechanisms and structure-activity relationships
-
Ferriola, P.C.; Cody, V.; Middleton, E. Protein kinase C inhibition by plant flavonoids: kinetic mechanisms and structure-activity relationships. Biochem. Pharmacol., 1989, 38, 1617-1624.
-
(1989)
Biochem. Pharmacol
, vol.38
, pp. 1617-1624
-
-
Ferriola, P.C.1
Cody, V.2
Middleton, E.3
-
150
-
-
0024453108
-
Inhibition of protein-tyrosine kinase activity by flavanoids and related compounds
-
Geahlen, R.L.; Koonchanok, N.M.; McLaughlin, J.L. Inhibition of protein-tyrosine kinase activity by flavanoids and related compounds. J. Nat. Prod., 1989, 52, 982-986.
-
(1989)
J. Nat. Prod
, vol.52
, pp. 982-986
-
-
Geahlen, R.L.1
Koonchanok, N.M.2
McLaughlin, J.L.3
-
151
-
-
0028104631
-
Synthesis and biochemical evaluation of a series of aminoflavones as potential inhibitors of protein tyrosine kinases p56lck, EGFr, and p60v-src
-
Cushman, M.; Zhu, H.; Geahlen, R.L.; Kraker, A.J. Synthesis and biochemical evaluation of a series of aminoflavones as potential inhibitors of protein tyrosine kinases p56lck, EGFr, and p60v-src. J. Med. Chem., 1994, 37, 3353-3362.
-
(1994)
J. Med. Chem
, vol.37
, pp. 3353-3362
-
-
Cushman, M.1
Zhu, H.2
Geahlen, R.L.3
Kraker, A.J.4
-
152
-
-
0037431421
-
Kinase inhibitors: Not just for kinases anymore
-
McGovern, S.L.; Shoichet, B.K. Kinase inhibitors: not just for kinases anymore. J. Med. Chem., 2003, 46, 1478-1483.
-
(2003)
J. Med. Chem
, vol.46
, pp. 1478-1483
-
-
McGovern, S.L.1
Shoichet, B.K.2
-
153
-
-
0141792701
-
A specific mechanism of non-specific inhibition
-
McGovern, S.L.; Helfand, B.T.; Feng, B.; Shoichet, B.K. A specific mechanism of non-specific inhibition. J. Med. Chem., 2003, 46, 4265-4272.
-
(2003)
J. Med. Chem
, vol.46
, pp. 4265-4272
-
-
McGovern, S.L.1
Helfand, B.T.2
Feng, B.3
Shoichet, B.K.4
-
154
-
-
0023924162
-
An antiinflammatory and immunomodulatory piperidinylbenzopyranone from Dysoxylum binectariferum: Isolation, structure and total synthesis
-
Naik, R.G.; Kattige, S.L.; Bhat, S.V.; Alreja, B.; deSousa, N.J.; Rupp, R.H. An antiinflammatory and immunomodulatory piperidinylbenzopyranone from Dysoxylum binectariferum: Isolation, structure and total synthesis. Tetrahedron, 1988, 44, 2081-2086.
-
(1988)
Tetrahedron
, vol.44
, pp. 2081-2086
-
-
Naik, R.G.1
Kattige, S.L.2
Bhat, S.V.3
Alreja, B.4
deSousa, N.J.5
Rupp, R.H.6
-
155
-
-
3042536038
-
Preclinical and clinical development of the cyclin-dependent kinase inhibitor
-
Shapiro, G.I. Preclinical and clinical development of the cyclin-dependent kinase inhibitor Flavopiridol. Clin. Cancer Res., 2004, 10 (12), 4270-4275.
-
(2004)
Flavopiridol. Clin. Cancer Res
, vol.10
, Issue.12
, pp. 4270-4275
-
-
Shapiro, G.I.1
-
156
-
-
0034597571
-
Thio-and oxoflavopiridols, cyclin-dependent kinase 1-. selective inhibitors: Synthesis and biological effects
-
Kim, K.S.; Sack, J.S.; Tokarski, J.S.; Qian, L.; Chao, S.T.; Leith, L.; Kelly, Y.F.; Misra, R.N.; Hunt, J.T.; Kimball, S.D.; Humphreys, W.G.; Wautlet, B.S.; Mulheron, J.G.; Webster, K.R. Thio-and oxoflavopiridols, cyclin-dependent kinase 1-. selective inhibitors: synthesis and biological effects. J. Med. Chem., 2000, 43, 4126-4134.
-
(2000)
J. Med. Chem.
, vol.43
, pp. 4126-4134
-
-
Kim, K.S.1
Sack, J.S.2
Tokarski, J.S.3
Qian, L.4
Chao, S.T.5
Leith, L.6
Kelly, Y.F.7
Misra, R.N.8
Hunt, J.T.9
Kimball, S.D.10
Humphreys, W.G.11
Wautlet, B.S.12
Mulheron, J.G.13
Webster, K.R.14
-
157
-
-
0029993339
-
Structural basis for specificity and potency of a flavonoid inhibitor of human CDK2, a cell cycle kinase
-
De Azevedo, W.F.; Muller-Dieckmann, H.J.; Schulze Gahmen, U.; Worland, P.J.; Sausville, E.; Kim, S.H. Structural basis for specificity and potency of a flavonoid inhibitor of human CDK2, a cell cycle kinase. Proc. Nat. Acad. Sci. USA., 1996, 93, 2735-2740.
-
(1996)
Proc. Nat. Acad. Sci. USA.
, vol.93
, pp. 2735-2740
-
-
de Azevedo, W.F.1
Muller-Dieckmann, H.J.2
Schulze Gahmen, U.3
Worland, P.J.4
Sausville, E.5
Kim, S.H.6
-
158
-
-
0031028163
-
Inhibition of cyclindependent kinases by purine analogs: Crystal structure of human cdk2 complexed with roscovitine
-
Azevedo, W.F.; Leclerc, S.; Meijer, L.; Havlicek, L.; Strnad, M.; Kim, S.H. Inhibition of cyclindependent kinases by purine analogs: crystal structure of human cdk2 complexed with roscovitine. Eur. J. Biochem., 1997, 243, 518-526.
-
(1997)
Eur. J. Biochem
, vol.243
, pp. 518-526
-
-
Azevedo, W.F.1
Leclerc, S.2
Meijer, L.3
Havlicek, L.4
Strnad, M.5
Kim, S.H.6
-
159
-
-
0035924235
-
Structure-based generation of a new class of potent Cdk4 inhibitors: New de Novo design strategy and library design
-
Honma, T.; Hayashi, K.; Aoyama, T.; Hashimoto, N.; Machida, T.; Fukasawa, K.; Iwama, T.; Ikeura, C.; Ikuta, M.; Suzuki-Takahashi, I.; Iwasawa, Y.; Hayama, T.; Nishimura, S.; Morishima, H. Structure-based generation of a new class of potent Cdk4 inhibitors: New de Novo design strategy and library design. J. Med. Chem., 2001, 44, 4615-4627.
-
(2001)
J. Med. Chem
, vol.44
, pp. 4615-4627
-
-
Honma, T.1
Hayashi, K.2
Aoyama, T.3
Hashimoto, N.4
McHida, T.5
Fukasawa, K.6
Iwama, T.7
Ikeura, C.8
Ikuta, M.9
Suzuki-Takahashi, I.10
Iwasawa, Y.11
Hayama, T.12
Nishimura, S.13
Morishima, H.14
-
160
-
-
13444311605
-
Crystal structure of a human cyclindependent kinase 6 complex with a flavonol inhibitor, fisetin
-
Lu, H.; Chang, D.J.; Baratte, B.; Meijer, L.; Schulze-Gahmen, U. Crystal structure of a human cyclindependent kinase 6 complex with a flavonol inhibitor, fisetin. J. Med. Chem., 2005, 48, 737-743.
-
(2005)
J. Med. Chem
, vol.48
, pp. 737-743
-
-
Lu, H.1
Chang, D.J.2
Baratte, B.3
Meijer, L.4
Schulze-Gahmen, U.5
-
161
-
-
0035959447
-
β-Turn mimetic library synthesis: Scaffolds and applications
-
Souers, A.J.; Ellman, J.A. β-Turn mimetic library synthesis: scaffolds and applications. Tetrahedron, 2001, 57, 7431-7448.
-
(2001)
Tetrahedron
, vol.57
, pp. 7431-7448
-
-
Souers, A.J.1
Ellman, J.A.2
-
162
-
-
0030768259
-
Design and synthesis of conformationally constrained amino acids as versatile scaffolds and peptide mimetics
-
Hanessian, C.; McNaughton,-Smith, G.; Lombart, H.G.; Lubell, W.D. Design and synthesis of conformationally constrained amino acids as versatile scaffolds and peptide mimetics. Tetrahedron, 1997, 53, 12789-12854.
-
(1997)
Tetrahedron
, vol.53
, pp. 12789-12854
-
-
Hanessian, C.1
McNaughton-Smith, G.2
Lombart, H.G.3
Lubell, W.D.4
-
163
-
-
0025156939
-
Cyclic pentapeptides as models for reverse turns: Determination of the equilibrium distribution between type I and type II conformations of Pro-Asn and Pro-Ala PP-turns
-
Stradley, S.J.; Rizo, J.; Bruch, M.D.; Stroup, A.N.; Gierasch, L.M. Cyclic pentapeptides as models for reverse turns: determination of the equilibrium distribution between type I and type II conformations of Pro-Asn and Pro-Ala PP-turns. Biopolymers, 1990, 29, 263-287.
-
(1990)
Biopolymers
, vol.29
, pp. 263-287
-
-
Stradley, S.J.1
Rizo, J.2
Bruch, M.D.3
Stroup, A.N.4
Gierasch, L.M.5
-
164
-
-
0033541091
-
Identification of a potent heterocyclic ligand to somatostatin receptor subtype 5 by the synthesis and screening of ll-turn mimetic libraries
-
Souers, A.J.; Virgilio, A.A.; Rosenquist, A.; Fenuik, W.; Ellman, J.A. Identification of a potent heterocyclic ligand to somatostatin receptor subtype 5 by the synthesis and screening of ll-turn mimetic libraries. J. Am. Chem. Soc., 1999, 121, 1817-1825.
-
(1999)
J. Am. Chem. Soc.
, vol.121
, pp. 1817-1825
-
-
Souers, A.J.1
Virgilio, A.A.2
Rosenquist, A.3
Fenuik, W.4
Ellman, J.A.5
-
165
-
-
0032497423
-
Novel inhibitors of 4441 integrin receptor interactions through library synthesis and screening
-
Souers, A.J.; Virgilio, A.A.; Schurer, S.S.; Ellmann, J.A. Novel inhibitors of 4441 integrin receptor interactions through library synthesis and screening. Bioorg. Med. Chem. Lett., 1998, 8, 2297-2302.
-
(1998)
Bioorg. Med. Chem. Lett
, vol.8
, pp. 2297-2302
-
-
Souers, A.J.1
Virgilio, A.A.2
Schurer, S.S.3
Ellmann, J.A.4
-
166
-
-
0036589386
-
Exploring privileged structures: The combinatorial synthesis of cyclic peptides
-
Horton, D.A.; Bourne, G.T.; Smythe, M.L. Exploring privileged structures: the combinatorial synthesis of cyclic peptides. J. Comp. Aided Mol. Drug Des., 2002, 16, 415-431.
-
(2002)
J. Comp. Aided Mol. Drug Des
, vol.16
, pp. 415-431
-
-
Horton, D.A.1
Bourne, G.T.2
Smythe, M.L.3
-
167
-
-
0032030723
-
Targeted molecular diversity in drug discovery: Integration of structure-based design and combinatorial chemistry
-
Li, J.; Murray, C.W.; Waszkowycz, B.; Young, S.C. Targeted molecular diversity in drug discovery: integration of structure-based design and combinatorial chemistry. Drug Discov. Today, 1998, 3, 105-118.
-
(1998)
Drug Discov. Today
, vol.3
, pp. 105-118
-
-
Li, J.1
Murray, C.W.2
Waszkowycz, B.3
Young, S.C.4
-
168
-
-
14644431688
-
Combinatorial approaches towards the discovery of new tryptase inhibitors
-
del Fresno, M.; Fernandez-Forner, D.; Miralpeix, M.; Segarra, V.; Ryder, H.; Royo, M.; Albericio, F. Combinatorial approaches towards the discovery of new tryptase inhibitors. Bioorg. Med. Chem. Lett., 2005, 15, 1659-1664.
-
(2005)
Bioorg. Med. Chem. Lett
, vol.15
, pp. 1659-1664
-
-
del Fresno, M.1
Fernandez-Forner, D.2
Miralpeix, M.3
Segarra, V.4
Ryder, H.5
Royo, M.6
Albericio, F.7
-
169
-
-
0037170771
-
Bivalent inhibition of ii-Tryptase: Distance scan of neighboring subunits by dibasic inhibitors
-
Schaschke, N.; Dominik, A.; Mastchiner, G.; Sommerhoff, C.P. Bivalent inhibition of ii-Tryptase: distance scan of neighboring subunits by dibasic inhibitors. Bioorg. Med. Chem. Lett., 2002, 12, 985-988.
-
(2002)
Bioorg. Med. Chem. Lett
, vol.12
, pp. 985-988
-
-
Schaschke, N.1
Dominik, A.2
Mastchiner, G.3
Sommerhoff, C.P.4
-
170
-
-
0035888142
-
Olid-phase syntheses of constrained RGD scaffolds and their binding to the FFvvv3 integrin receptor
-
Royo, M.; Van Den Nest, W.; del Fresno, M.; Frieden, A.; Yahalom, D.; Rosenblatt, M.; Chorev, M.; Albericio, F. olid-phase syntheses of constrained RGD scaffolds and their binding to the FFvvv3 integrin receptor. Tetrahedron Lett., 2001, 42, 7387-7391.
-
(2001)
Tetrahedron Lett.
, vol.42
, pp. 7387-7391
-
-
Royo, M.1
van den Nest, W.2
del Fresno, M.3
Frieden, A.4
Yahalom, D.5
Rosenblatt, M.6
Chorev, M.7
Albericio, F.8
-
171
-
-
0028031720
-
Design and synthesis of peptidomimetic inhibitors of HIV-1 protease and renin: Evidence for improved transport
-
Smith, A.B.; Hirschmann, R.; Pasternak, A.; Akaishi, R.; Guzman, M.C.; Jones, D.R.; Keenan, T.P.; Sprengler, P.A.; Darke, P.L.; Emini, E.A.; Holloway, M.K.; Schleif, W.A. Design and synthesis of peptidomimetic inhibitors of HIV-1 protease and renin: evidence for improved transport. J. Med. Chem., 1994, 37, 215-218.
-
(1994)
J. Med. Chem
, vol.37
, pp. 215-218
-
-
Smith, A.B.1
Hirschmann, R.2
Pasternak, A.3
Akaishi, R.4
Guzman, M.C.5
Jones, D.R.6
Keenan, T.P.7
Sprengler, P.A.8
Darke, P.L.9
Emini, E.A.10
Holloway, M.K.11
Schleif, W.A.12
-
172
-
-
0030806489
-
An orally bioavailable pyrrolinone inhibitor of HIV-1 protease: Computational analysis and X-ray crystal structure of the enzyme complex
-
Smith, A.B.; Hirschmann, R.; Pasternack, A.; Yao, W.; Sprengeler, P.A.; Holloway, M.K.; Kuo, L.C.; Chen, Z.; Darke, P.L.; Schleif, W.A. An orally bioavailable pyrrolinone inhibitor of HIV-1 protease: computational analysis and X-ray crystal structure of the enzyme complex. J. Med. Chem., 1997, 40, 2440-2444.
-
(1997)
J. Med. Chem
, vol.40
, pp. 2440-2444
-
-
Smith, A.B.1
Hirschmann, R.2
Pasternack, A.3
Yao, W.4
Sprengeler, P.A.5
Holloway, M.K.6
Kuo, L.C.7
Chen, Z.8
Darke, P.L.9
Schleif, W.A.10
-
173
-
-
0028882977
-
Pyrrolinone-based HIV protease inhibitors: Design, synthesis, and antiviral activity: Evidence for improved transport
-
Smith, A.B.; Hirschmann, R.; Pasternak, A.; Guzman, M.C.; Yokoyama, A.; Sprengeler, P.A.; Darke, P.L.; Emini, E.A.; Schleif, W.A. Pyrrolinone-based HIV protease inhibitors: design, synthesis, and antiviral activity: Evidence for improved transport. J. Am. Chem. Soc., 1995, 117, 11113-11123.
-
(1995)
J. Am. Chem. Soc
, vol.117
, pp. 11113-11123
-
-
Smith, A.B.1
Hirschmann, R.2
Pasternak, A.3
Guzman, M.C.4
Yokoyama, A.5
Sprengeler, P.A.6
Darke, P.L.7
Emini, E.A.8
Schleif, W.A.9
-
174
-
-
0028941674
-
Design and synthesis of nonpeptide peptidomimetic inhibitors of renin
-
Smith, A.B.; Akaishi, R.; Jones, D.R.; Keenan, T.P.; Guzman, M.C.; Holcomb, R.C.; Sprengeler, P.A.; Wood, J.L.; Hirschmann, R.; Holloway, M.K. Design and synthesis of nonpeptide peptidomimetic inhibitors of renin. Biopolymers, 1995, 37, 29-53.
-
(1995)
Biopolymers
, vol.37
, pp. 29-53
-
-
Smith, A.B.1
Akaishi, R.2
Jones, D.R.3
Keenan, T.P.4
Guzman, M.C.5
Holcomb, R.C.6
Sprengeler, P.A.7
Wood, J.L.8
Hirschmann, R.9
Holloway, M.K.10
-
175
-
-
0034736381
-
Design, synthesis, and evaluation of a pyrrolinone-based matrix metalloprotease inhibitor
-
Smith, A.B.; Nittoli, T.; Sprengeler, P.A.; Duan, J.J.-W.; Liu, R.-Q.; Hirschmann, R.F. Design, synthesis, and evaluation of a pyrrolinone-based matrix metalloprotease inhibitor. Org. Lett., 2000, 2, 3809-3812.
-
(2000)
Org. Lett.
, vol.2
, pp. 3809-3812
-
-
Smith, A.B.1
Nittoli, T.2
Sprengeler, P.A.3
Duan, J.J.-W.4
Liu, R.-Q.5
Hirschmann, R.F.6
-
176
-
-
0033552280
-
Design and synthesis of a competent pyrrolinone-peptide hybrid ligand for the Class II Major Histocompatibility Complex Protein HLA-DR1
-
Smith, A.B.; Benowitz, A.B.; Sprengeler, P.A.; Barbosa, J.; Guzman, M.C.; Hirschmann, R.; Schweiger, E.J.; Bolin, D.R.; Nagy, Z.; Campbell, R.M.; Cox, D.C.; Olson, G.L. Design and synthesis of a competent pyrrolinone-peptide hybrid ligand for the Class II Major Histocompatibility Complex Protein HLA-DR1. J. Am. Chem. Soc., 1999, 121, 9286-9298.
-
(1999)
J. Am. Chem. Soc
, vol.121
, pp. 9286-9298
-
-
Smith, A.B.1
Benowitz, A.B.2
Sprengeler, P.A.3
Barbosa, J.4
Guzman, M.C.5
Hirschmann, R.6
Schweiger, E.J.7
Bolin, D.R.8
Nagy, Z.9
Campbell, R.M.10
Cox, D.C.11
Olson, G.L.12
-
177
-
-
13844276177
-
Design, synthesis, and binding affinities of pyrrolinone-based somatostatin mimetics
-
Smith, A.; Charnley, A.K.; Mesaros, E.F.; Kikuchi, O.; Wang, W.; Benowitz, A.; Chu, C.L.; Feng, J.J.; Chen, K.H.; Lin, A.; Cheng, F.C.; Taylor, L.; Hirschmann, R. Design, synthesis, and binding affinities of pyrrolinone-based somatostatin mimetics. Org. Lett., 2005, 7, 399-402.
-
(2005)
Org. Lett
, vol.7
, pp. 399-402
-
-
Smith, A.1
Charnley, A.K.2
Mesaros, E.F.3
Kikuchi, O.4
Wang, W.5
Benowitz, A.6
Chu, C.L.7
Feng, J.J.8
Chen, K.H.9
Lin, A.10
Cheng, F.C.11
Taylor, L.12
Hirschmann, R.13
-
178
-
-
0033011780
-
Molecular modeling, synthesis, and structures of N-methylated 3,5-linked pyrrolin-4-ones toward the creation of a privileged nonpeptide scaffold
-
Smith, A.B.; Favor, D.A.; Sprengeler, P.A.; Guzman, M.C.; Carroll, P-J.; Furst, G.T.; Hirschmann, R. Molecular modeling, synthesis, and structures of N-methylated 3,5-linked pyrrolin-4-ones toward the creation of a privileged nonpeptide scaffold. Bioorg. Med. Chem., 1999, 7, 9-22.
-
(1999)
Bioorg. Med. Chem.
, vol.7
, pp. 9-22
-
-
Smith, A.B.1
Favor, D.A.2
Sprengeler, P.A.3
Guzman, M.C.4
Carroll, P.-J.5
Furst, G.T.6
Hirschmann, R.7
-
179
-
-
3042799070
-
A planning strategy for diversity-oriented synthesis
-
Burke, M.D.; Schreiber, S.L. A planning strategy for diversity-oriented synthesis. Angew. Chem. Int. Ed. Engl., 2004, 43, 46-58.
-
(2004)
Angew. Chem. Int. Ed. Engl
, vol.43
, pp. 46-58
-
-
Burke, M.D.1
Schreiber, S.L.2
-
180
-
-
0142147275
-
Generating diverse skeletons of small molecules combinatorially
-
Burke, M.D.; Berger, E.M.; Schreiber, S.L. Generating diverse skeletons of small molecules combinatorially. Science, 2003, 302, 613-618.
-
(2003)
Science
, vol.302
, pp. 613-618
-
-
Burke, M.D.1
Berger, E.M.2
Schreiber, S.L.3
-
181
-
-
58149358949
-
Molecular diversity by design
-
Schreiber, S.L. Molecular diversity by design. Nature, 2009, 457, 153-154.
-
(2009)
Nature
, vol.457
, pp. 153-154
-
-
Schreiber, S.L.1
|