-
1
-
-
6444234760
-
The role of medicinal chemistry in drug discovery - then and now
-
Lombardino J.G., Lowe J.A. The role of medicinal chemistry in drug discovery - then and now. Nat. Rev. Drug Discov. 2004, 3:853-862.
-
(2004)
Nat. Rev. Drug Discov.
, vol.3
, pp. 853-862
-
-
Lombardino, J.G.1
Lowe, J.A.2
-
2
-
-
0034677966
-
Drug discovery: a historical perspective
-
Drews J. Drug discovery: a historical perspective. Science 2000, 287:1960-1963.
-
(2000)
Science
, vol.287
, pp. 1960-1963
-
-
Drews, J.1
-
3
-
-
84882483876
-
-
For example, during the first four years of the discovery campaign that led to cimetidine, some 200 compounds were synthesized and assessed. Ganellin, C. R. Discovery of the antiulcer drug tagamet. In Drug Discovery and Development (Chorghade, M. S., Ed.), John Wiley & Sons, Inc, Hoboken, New Jersey
-
For example, during the first four years of the discovery campaign that led to cimetidine, some 200 compounds were synthesized and assessed. Ganellin, C. R. Discovery of the antiulcer drug tagamet. In Drug Discovery and Development (Chorghade, M. S., Ed.), John Wiley & Sons, Inc, Hoboken, New Jersey, Vol. 1, p. 300.
-
, vol.1
, pp. 300
-
-
-
4
-
-
10844263277
-
Pharmacological screening tests
-
Smith W.G. Pharmacological screening tests. Progr. Med. Chem. 1964, 1:1-33.
-
(1964)
Progr. Med. Chem.
, vol.1
, pp. 1-33
-
-
Smith, W.G.1
-
5
-
-
0023713884
-
Drug discovery - today and tomorrow: the role of medicinal chemistry
-
Freter K.R. Drug discovery - today and tomorrow: the role of medicinal chemistry. Pharmaceut. Res. 1988, 5:397-400.
-
(1988)
Pharmaceut. Res.
, vol.5
, pp. 397-400
-
-
Freter, K.R.1
-
7
-
-
33646517064
-
Drug discovery: selecting the optimal approach
-
Sams-Dodd F. Drug discovery: selecting the optimal approach. Drug Discov. Today 2006, 11:465-472.
-
(2006)
Drug Discov. Today
, vol.11
, pp. 465-472
-
-
Sams-Dodd, F.1
-
8
-
-
0024146165
-
Cyclosporins, fungal metabolites with immunosuppressive activities
-
Von Wartburg A., Traber R. Cyclosporins, fungal metabolites with immunosuppressive activities. Progr. Med. Chem. 1988, 25:1-33.
-
(1988)
Progr. Med. Chem.
, vol.25
, pp. 1-33
-
-
Von Wartburg, A.1
Traber, R.2
-
9
-
-
0024959451
-
Peptidyl-prolyl cis-trans isomerase is the cyclosporin A-binding protein cyclophilin
-
Takahashi N., Hayano T., Suzuki M. Peptidyl-prolyl cis-trans isomerase is the cyclosporin A-binding protein cyclophilin. Nature 1989, 337:473-475.
-
(1989)
Nature
, vol.337
, pp. 473-475
-
-
Takahashi, N.1
Hayano, T.2
Suzuki, M.3
-
11
-
-
0036511069
-
Application of high-throughput, molecular-targeted screening to anticancer drug discovery
-
Shoemaker R.H., Scudiero D.A., Melillo G., Currens M.J., Monks A.P., Rabow A.A., Covell D.G., Sausville E.A. Application of high-throughput, molecular-targeted screening to anticancer drug discovery. Curr. Top. Med. Chem. 2002, 2:229-246.
-
(2002)
Curr. Top. Med. Chem.
, vol.2
, pp. 229-246
-
-
Shoemaker, R.H.1
Scudiero, D.A.2
Melillo, G.3
Currens, M.J.4
Monks, A.P.5
Rabow, A.A.6
Covell, D.G.7
Sausville, E.A.8
-
12
-
-
0038270983
-
Hydroxyurea, a new type of potential antitumor agent
-
Stearns B., Losee K.A., Bernstein J. Hydroxyurea, a new type of potential antitumor agent. J. Med. Chem. 1963, 6:201.
-
(1963)
J. Med. Chem.
, vol.6
, pp. 201
-
-
Stearns, B.1
Losee, K.A.2
Bernstein, J.3
-
13
-
-
73649185176
-
Experimental evaluation of potential anticancer agents. VIII. Effects of certain nitrosoureas on intracerebral L1210 leukemia
-
Schabel F.M., Johnston T.P., McCaleb G.S., Montgomery J.A., Laster W.R., Skipper H.E. Experimental evaluation of potential anticancer agents. VIII. Effects of certain nitrosoureas on intracerebral L1210 leukemia. Cancer Res. 1963, 23:725-733.
-
(1963)
Cancer Res.
, vol.23
, pp. 725-733
-
-
Schabel, F.M.1
Johnston, T.P.2
McCaleb, G.S.3
Montgomery, J.A.4
Laster, W.R.5
Skipper, H.E.6
-
14
-
-
0000741407
-
New inhibitor of monoamine oxidase
-
Taylor J.D., Wykes A.A., Gladish Y.C., Martin W.B. New inhibitor of monoamine oxidase. Nature 1960, 187:941.
-
(1960)
Nature
, vol.187
, pp. 941
-
-
Taylor, J.D.1
Wykes, A.A.2
Gladish, Y.C.3
Martin, W.B.4
-
15
-
-
0014596980
-
Chemotherapy and comparative biochemistry: G. H. A. Clowes memorial lecture
-
Hitchings G.H. Chemotherapy and comparative biochemistry: G. H. A. Clowes memorial lecture. Cancer Res. 1969, 29:1895-1903.
-
(1969)
Cancer Res.
, vol.29
, pp. 1895-1903
-
-
Hitchings, G.H.1
-
16
-
-
0031024171
-
Experimental and computational approaches to estimate solubility and permeability in drug discovery and development settings
-
Lipinski C.A., Lombardo F., Dominy B.W., Feeney P.J. Experimental and computational approaches to estimate solubility and permeability in drug discovery and development settings. Adv. Drug Deliv. Rev. 1997, 23:3-25.
-
(1997)
Adv. Drug Deliv. Rev.
, vol.23
, pp. 3-25
-
-
Lipinski, C.A.1
Lombardo, F.2
Dominy, B.W.3
Feeney, P.J.4
-
17
-
-
0034461768
-
Drug-like properties and the causes of poor solubility and poor permeability
-
Lipinski C.A. Drug-like properties and the causes of poor solubility and poor permeability. J. Pharmacol. Toxicol. Meth. 2001, 44:235-249.
-
(2001)
J. Pharmacol. Toxicol. Meth.
, vol.44
, pp. 235-249
-
-
Lipinski, C.A.1
-
18
-
-
0037468884
-
A comparison of physiochemical property profiles of development and marketed oral drugs
-
Wenlock M.C., Austin R.P., Barton P., Davis A.M., Leeson P.D. A comparison of physiochemical property profiles of development and marketed oral drugs. J. Med. Chem. 2003, 46:1250-1256.
-
(2003)
J. Med. Chem.
, vol.46
, pp. 1250-1256
-
-
Wenlock, M.C.1
Austin, R.P.2
Barton, P.3
Davis, A.M.4
Leeson, P.D.5
-
19
-
-
0033576601
-
The design of leadlike combinatorial libraries
-
Teague S.J., Davis A.M., Leeson P.D., Oprea T. The design of leadlike combinatorial libraries. Angew. Chem. Int. Ed. 1999, 38:3742-3748.
-
(1999)
Angew. Chem. Int. Ed.
, vol.38
, pp. 3742-3748
-
-
Teague, S.J.1
Davis, A.M.2
Leeson, P.D.3
Oprea, T.4
-
20
-
-
0035324944
-
Molecular complexity and the impact on finding leads for drug discovery
-
Hann M.M., Leach A.R., Harper G. Molecular complexity and the impact on finding leads for drug discovery. J. Chem. Inform. Comput. Sci. 2001, 41:856-864.
-
(2001)
J. Chem. Inform. Comput. Sci.
, vol.41
, pp. 856-864
-
-
Hann, M.M.1
Leach, A.R.2
Harper, G.3
-
21
-
-
0036589285
-
Current trends in lead discovery: Are we looking for the appropriate properties?
-
Oprea T. Current trends in lead discovery: Are we looking for the appropriate properties?. J. Comput.-Aided Mol. Des. 2002, 16:325-334.
-
(2002)
J. Comput.-Aided Mol. Des.
, vol.16
, pp. 325-334
-
-
Oprea, T.1
-
23
-
-
12844283957
-
High-throughput drug discovery: What can we expect from HTS?
-
Gribbon P., Sewing A. High-throughput drug discovery: What can we expect from HTS?. Drug Discov. Today 2005, 10:17-22.
-
(2005)
Drug Discov. Today
, vol.10
, pp. 17-22
-
-
Gribbon, P.1
Sewing, A.2
-
24
-
-
0038387389
-
A guide to drug discovery: Hit and lead generation: beyond high-throughput screening
-
Bleicher K.H., Böhm H.J., Müller K., Alanine A.I. A guide to drug discovery: Hit and lead generation: beyond high-throughput screening. Nat. Rev. Drug Discov 2003, 2:369-378.
-
(2003)
Nat. Rev. Drug Discov
, vol.2
, pp. 369-378
-
-
Bleicher, K.H.1
Böhm, H.J.2
Müller, K.3
Alanine, A.I.4
-
26
-
-
0034093179
-
Quantized surface complementarity diversity (QSCD): a model based small molecule-target complementarity
-
Wintner E.A., Moallemi C.C. Quantized surface complementarity diversity (QSCD): a model based small molecule-target complementarity. J. Med. Chem. 2000, 43:1993-2006.
-
(2000)
J. Med. Chem.
, vol.43
, pp. 1993-2006
-
-
Wintner, E.A.1
Moallemi, C.C.2
-
27
-
-
33645366993
-
Defining and maintaining a high quality screening collection: the GSK experience
-
Lane S.J., Eggleston D.S., Brinded K.A., Hollerton J.C., Taylor N.L., Readshaw S.A. Defining and maintaining a high quality screening collection: the GSK experience. Drug Discov. Today 2006, 11:267-272.
-
(2006)
Drug Discov. Today
, vol.11
, pp. 267-272
-
-
Lane, S.J.1
Eggleston, D.S.2
Brinded, K.A.3
Hollerton, J.C.4
Taylor, N.L.5
Readshaw, S.A.6
-
28
-
-
19944405127
-
Components of successful lead generation
-
Davis A.M., Keeling D.J., Steele J., Tomkinson N.P., Tinker A.C. Components of successful lead generation. Curr. Top. Med. Chem. 2005, 5:421-439.
-
(2005)
Curr. Top. Med. Chem.
, vol.5
, pp. 421-439
-
-
Davis, A.M.1
Keeling, D.J.2
Steele, J.3
Tomkinson, N.P.4
Tinker, A.C.5
-
29
-
-
84882526755
-
Compound collections: acquisition, annotation and access
-
The Royal Society of Chemistry, Cambridge, P.A. Bartlett, M. Entzeroth (Eds.)
-
Richardson R. Compound collections: acquisition, annotation and access. Exploiting Chemical Diversity for Drug Discovery 2006, 113-136. The Royal Society of Chemistry, Cambridge. P.A. Bartlett, M. Entzeroth (Eds.).
-
(2006)
Exploiting Chemical Diversity for Drug Discovery
, pp. 113-136
-
-
Richardson, R.1
-
30
-
-
0345511077
-
-
Supplement
-
Anon Nature 1996, 384:1-5. Supplement.
-
(1996)
Nature
, vol.384
, pp. 1-5
-
-
Anon1
-
31
-
-
0033003760
-
A simple statistical parameter for use in evaluation and validation of high throughput screening assays
-
Zhang J-H., Chung T.D.Y., Oldenburg K.R. A simple statistical parameter for use in evaluation and validation of high throughput screening assays. J. Biomol. Screen 1999, 4:67-73.
-
(1999)
J. Biomol. Screen
, vol.4
, pp. 67-73
-
-
Zhang, J.-H.1
Chung, T.D.Y.2
Oldenburg, K.R.3
-
32
-
-
0037439447
-
Nonleadlikeness and leadlikeness in biochemical screening
-
Rishton G.M. Nonleadlikeness and leadlikeness in biochemical screening. Drug Discov. Today 2002, 8:86-96.
-
(2002)
Drug Discov. Today
, vol.8
, pp. 86-96
-
-
Rishton, G.M.1
-
33
-
-
33745381593
-
An empirical process for the design of high-throughput screening deck filters
-
Pearce B.C., Sofia M.J., Good A.C., Drexler D.M., Stock D.A. An empirical process for the design of high-throughput screening deck filters. J. Chem. Inform. Model 2006, 46:1060-1068.
-
(2006)
J. Chem. Inform. Model
, vol.46
, pp. 1060-1068
-
-
Pearce, B.C.1
Sofia, M.J.2
Good, A.C.3
Drexler, D.M.4
Stock, D.A.5
-
34
-
-
0033194752
-
Strategic pooling of compounds for high-throughput screening
-
Hann M., Hudson B., Lewell X., Lifely R., Miller L., Ramsden N. Strategic pooling of compounds for high-throughput screening. J. Chem. Inform. Comp. Sci. 1999, 39:897-902.
-
(1999)
J. Chem. Inform. Comp. Sci.
, vol.39
, pp. 897-902
-
-
Hann, M.1
Hudson, B.2
Lewell, X.3
Lifely, R.4
Miller, L.5
Ramsden, N.6
-
35
-
-
33745188660
-
Screening in a spirit haunted world
-
Soichet B.K. Screening in a spirit haunted world. Drug Discov. Today 2006, 11:607-615.
-
(2006)
Drug Discov. Today
, vol.11
, pp. 607-615
-
-
Soichet, B.K.1
-
36
-
-
0037061628
-
A common mechanism underlying promiscuous inhibitors from virtual and high-throughput screening
-
McGovern S.L., Caselli E., Grigorieff N., Shoichet B.K. A common mechanism underlying promiscuous inhibitors from virtual and high-throughput screening. J. Med. Chem. 2002, 45:1712-1722.
-
(2002)
J. Med. Chem.
, vol.45
, pp. 1712-1722
-
-
McGovern, S.L.1
Caselli, E.2
Grigorieff, N.3
Shoichet, B.K.4
-
37
-
-
0037011890
-
Development of a virtual screening method for identification of quot;frequent hitters quot; in compound libraries
-
Roche O., Schneider P., Zuegge J., Guba W., Kansy M., Alanine A., Bleicher K., Danel F., Gutknecht E.-M., Rogers-Evans M., Neidhart W., Stalder H., Dillon M., Sjoegren E., Fotouhi N., Gillespie P., Goodnow R., Harris W., Jones P., Taniguchi M., Tsujii S., von Saal W., Zimmermann G., Schneider G. Development of a virtual screening method for identification of "frequent hitters" in compound libraries. J. Med. Chem. 2002, 45:137-142.
-
(2002)
J. Med. Chem.
, vol.45
, pp. 137-142
-
-
Roche, O.1
Schneider, P.2
Zuegge, J.3
Guba, W.4
Kansy, M.5
Alanine, A.6
Bleicher, K.7
Danel, F.8
Gutknecht, E.-M.9
Rogers-Evans, M.10
Neidhart, W.11
Stalder, H.12
Dillon, M.13
Sjoegren, E.14
Fotouhi, N.15
Gillespie, P.16
Goodnow, R.17
Harris, W.18
Jones, P.19
Taniguchi, M.20
Tsujii, S.21
von Saal, W.22
Zimmermann, G.23
Schneider, G.24
more..
-
38
-
-
33645887230
-
Critical review of the role of HTS in drug discovery
-
Macarron R. Critical review of the role of HTS in drug discovery. Drug Discov. Today 2006, 11:277-279.
-
(2006)
Drug Discov. Today
, vol.11
, pp. 277-279
-
-
Macarron, R.1
-
39
-
-
33746294770
-
The hit-to-lead process at Schering AG: strategic aspects
-
Steinmeyer A. The hit-to-lead process at Schering AG: strategic aspects. ChemMedChem 2006, 1:31-36.
-
(2006)
ChemMedChem
, vol.1
, pp. 31-36
-
-
Steinmeyer, A.1
-
40
-
-
33644867602
-
Improving the hit-to-lead process: data-driven assessment of drug-like and lead-like screening hits
-
Wunberg T., Hendrix M., Hillisch A., Lobell M., Meier H., Schmeck C., Wild H., Hinzen B. Improving the hit-to-lead process: data-driven assessment of drug-like and lead-like screening hits. Drug Discov. Today 2006, 11:175-180.
-
(2006)
Drug Discov. Today
, vol.11
, pp. 175-180
-
-
Wunberg, T.1
Hendrix, M.2
Hillisch, A.3
Lobell, M.4
Meier, H.5
Schmeck, C.6
Wild, H.7
Hinzen, B.8
-
41
-
-
2342528574
-
Hit-to-lead studies: the discovery of potent, orally active, thiophenecarboxamide IKK-2 inhibitors
-
Baxter A., Brough S., Cooper A., Floettmann E., Foster S., Harding C., Kettle J., McInally T., Martin C., Mobbs M., Needham M., Newham P., Paine S., St-Gallay S., Salter S., Unitt J., Xue Y. Hit-to-lead studies: the discovery of potent, orally active, thiophenecarboxamide IKK-2 inhibitors. Bioorg. Med. Chem. Lett. 2004, 14:2817-2822.
-
(2004)
Bioorg. Med. Chem. Lett.
, vol.14
, pp. 2817-2822
-
-
Baxter, A.1
Brough, S.2
Cooper, A.3
Floettmann, E.4
Foster, S.5
Harding, C.6
Kettle, J.7
McInally, T.8
Martin, C.9
Mobbs, M.10
Needham, M.11
Newham, P.12
Paine, S.13
St-Gallay, S.14
Salter, S.15
Unitt, J.16
Xue, Y.17
-
42
-
-
0033102135
-
Renin inhibition by substituted piperidines: A novel paradigm for the inhibition of monomeric aspartic proteinases?
-
Oefner C., Binggeli A., Breu V., Bur D., Clozel J-P., D'Arcy A., Dorn A., Fischli W., Grüninger F., Güller G.Hirth R., Märki H.P., Mathews S., Müller M., Ridley R.G., Stadier H., Vieira E., Wilhelm M., Winkler F.K., Wostl W. Renin inhibition by substituted piperidines: A novel paradigm for the inhibition of monomeric aspartic proteinases?. Chem. Biol. 1999, 6:127-131.
-
(1999)
Chem. Biol.
, vol.6
, pp. 127-131
-
-
Oefner, C.1
Binggeli, A.2
Breu, V.3
Bur, D.4
Clozel, J.-P.5
D'Arcy, A.6
Dorn, A.7
Fischli, W.8
Grüninger, F.9
Güller, G.10
Hirth, R.11
Märki, H.P.12
Mathews, S.13
Müller, M.14
Ridley, R.G.15
Stadier, H.16
Vieira, E.17
Wilhelm, M.18
Winkler, F.K.19
Wostl, W.20
more..
-
43
-
-
84882514656
-
-
US 4,093,805 (1978 to Dow Chemical Co.)
-
Britton, T. C., Trepanier, D. L. 4-Hydroxy-3,4-dihydro-2(1H)-quinazolinethiones. US 4,093,805 (1978 to Dow Chemical Co.).
-
4-Hydroxy-3,4-dihydro-2(1H)-quinazolinethiones
-
-
Britton, T.C.1
Trepanier, D.L.2
-
45
-
-
84882479009
-
-
Preparation of pharmaceutically active heterocyclic amines and their use for treating head injury, spinal trauma, stroke, etc. WO8808424 (1988 Upjohn Co.)
-
McCall, J. M., Ayer, D. E., Jacobsen, E. J., Van Doornik, F. J., Palmer, J. R. Preparation of pharmaceutically active heterocyclic amines and their use for treating head injury, spinal trauma, stroke, etc. WO8808424 (1988 Upjohn Co.).
-
-
-
McCall, J.M.1
Ayer, D.E.2
Jacobsen, E.J.3
Van Doornik, F.J.4
Palmer, J.R.5
-
46
-
-
0025740266
-
Novel non-nucleoside inhibitors of HIV-1 reverse transcriptase.1. Tricyclic pyridobenzo- and dipyridodiazepinones
-
Hargrave K.D., Proudfoot J.R., Grozinger K.G., Cullen E., Kapadia S.R., Patel U.R., Fuchs V.U., Mauldin S.C., Vitous J., Behnke M.L., Klunder J.M., Pal K., Skiles J.W., McNeil D.W., Rose J.M., Chow G.C., Skoog M.T., Wu J.C., Schmidt G., Engel W.W., Eberlein W.G., Saboe T.D., Campbell S.J., Rosenthal A.S., Adams J. Novel non-nucleoside inhibitors of HIV-1 reverse transcriptase.1. Tricyclic pyridobenzo- and dipyridodiazepinones. J. Med. Chem. 1991, 34:2231-2241.
-
(1991)
J. Med. Chem.
, vol.34
, pp. 2231-2241
-
-
Hargrave, K.D.1
Proudfoot, J.R.2
Grozinger, K.G.3
Cullen, E.4
Kapadia, S.R.5
Patel, U.R.6
Fuchs, V.U.7
Mauldin, S.C.8
Vitous, J.9
Behnke, M.L.10
Klunder, J.M.11
Pal, K.12
Skiles, J.W.13
McNeil, D.W.14
Rose, J.M.15
Chow, G.C.16
Skoog, M.T.17
Wu, J.C.18
Schmidt, G.19
Engel, W.W.20
Eberlein, W.G.21
Saboe, T.D.22
Campbell, S.J.23
Rosenthal, A.S.24
Adams, J.25
more..
-
47
-
-
0028823979
-
Novel non-nucleoside inhibitors of HIV-1 reverse transcriptase. 4. 2-Substituted dipyridodiazepinones are potent inhibitors of both wild type and cysteine-181 HIV-1 reverse transcriptase enzymes
-
Proudfoot J.R., Hargrave K.D., Kapadia S.R., Patel U.R., Grozinger K.G., McNeil D.W., Cullen E., Cardozo M., Tong L., Kelly T.A., Rose J., David E., Mauldin S.C., Fuchs V.U., Vitous J., Hoermann M., Klunder J.M., Raghavan P., Skiles J.W., Mui P., Richman D.D., Sullivan J.L., Shih C.-K., Grob P., Adams J. Novel non-nucleoside inhibitors of HIV-1 reverse transcriptase. 4. 2-Substituted dipyridodiazepinones are potent inhibitors of both wild type and cysteine-181 HIV-1 reverse transcriptase enzymes. J. Med. Chem. 1995, 38:4830-4838.
-
(1995)
J. Med. Chem.
, vol.38
, pp. 4830-4838
-
-
Proudfoot, J.R.1
Hargrave, K.D.2
Kapadia, S.R.3
Patel, U.R.4
Grozinger, K.G.5
McNeil, D.W.6
Cullen, E.7
Cardozo, M.8
Tong, L.9
Kelly, T.A.10
Rose, J.11
David, E.12
Mauldin, S.C.13
Fuchs, V.U.14
Vitous, J.15
Hoermann, M.16
Klunder, J.M.17
Raghavan, P.18
Skiles, J.W.19
Mui, P.20
Richman, D.D.21
Sullivan, J.L.22
Shih, C.-K.23
Grob, P.24
Adams, J.25
more..
-
48
-
-
15144354770
-
Novel nonnucleoside inhibitors of HIV-1 reverse transcriptase. 8. 8-Aryloxymethyl- and 8-arylthiomethyldipyridodiazepinones
-
Cywin C.L., Klunder J.M., Hoermann M., Brickwood J.R., David E., Grob P.M., Schwartz R., Pauletti D., Barringer K.J., Shih C.-K., Sorge C.L., Erickson D.A., Joseph D.P., Hattox S.E. Novel nonnucleoside inhibitors of HIV-1 reverse transcriptase. 8. 8-Aryloxymethyl- and 8-arylthiomethyldipyridodiazepinones. J. Med. Chem. 1998, 41:2972-2984.
-
(1998)
J. Med. Chem.
, vol.41
, pp. 2972-2984
-
-
Cywin, C.L.1
Klunder, J.M.2
Hoermann, M.3
Brickwood, J.R.4
David, E.5
Grob, P.M.6
Schwartz, R.7
Pauletti, D.8
Barringer, K.J.9
Shih, C.-K.10
Sorge, C.L.11
Erickson, D.A.12
Joseph, D.P.13
Hattox, S.E.14
-
49
-
-
0028337357
-
-
Chan M.F., Okun I., Stavros F.L., Hwang E. Biochem. Biophys. Res. Comm. 1994, 201:228-234.
-
(1994)
Biochem. Biophys. Res. Comm.
, vol.201
, pp. 228-234
-
-
Chan, M.F.1
Okun, I.2
Stavros, F.L.3
Hwang, E.4
-
50
-
-
0030598177
-
Halogen substitution at the isoxazole ring enhances the activity of N-(isoxazolyl)sulfonamide endothelin antagonists
-
Chan M.F., Raju B., Kois A., Castillo R.S., Verner E.J., Wu C., Hwang E., Okun I., Stavros F., Balaji V.N. Halogen substitution at the isoxazole ring enhances the activity of N-(isoxazolyl)sulfonamide endothelin antagonists. Bioorg. Med. Chem. Lett. 1996, 6:2393-2398.
-
(1996)
Bioorg. Med. Chem. Lett.
, vol.6
, pp. 2393-2398
-
-
Chan, M.F.1
Raju, B.2
Kois, A.3
Castillo, R.S.4
Verner, E.J.5
Wu, C.6
Hwang, E.7
Okun, I.8
Stavros, F.9
Balaji, V.N.10
-
52
-
-
0030943903
-
Discovery of TBC11251, a potent, long acting, orally active endothelin receptor-A selective antagonist
-
Wu C., Chan M.F., Stavros F., Raju B., Okun I., Mong S., Keller K.M., Brock T., Kogan T.P., Dixon R.A.F. Discovery of TBC11251, a potent, long acting, orally active endothelin receptor-A selective antagonist. J. Med. Chem. 1997, 40:1690-1697.
-
(1997)
J. Med. Chem.
, vol.40
, pp. 1690-1697
-
-
Wu, C.1
Chan, M.F.2
Stavros, F.3
Raju, B.4
Okun, I.5
Mong, S.6
Keller, K.M.7
Brock, T.8
Kogan, T.P.9
Dixon, R.A.F.10
-
53
-
-
0028203238
-
A antagonist 5-(dimethylamino)-N-(3,4-dimethyl-5- isoxazolyl)-1-naphthalenesulfonamide
-
A antagonist 5-(dimethylamino)-N-(3,4-dimethyl-5- isoxazolyl)-1-naphthalenesulfonamide. 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
Kozlowskil, M.17
-
54
-
-
0032542312
-
Biphenylsulfonamide endothelin antagonists: structure-activity relationships of a series of mono- and disubstituted analogues and pharmacology of the orally active endothelin antagonist 2'-Amino-N-(3,4-dimethyl-5-isoxazolyl)-4'-(2-methylpropyl)[1,1'-biphenyl ]-2-sulfonamide (BMS-187308)
-
Murugesan N., Gu Z., Stein P.D., Bisaha S., Spergel S., Girotra R., Lee V.G., Lloyd J., Misra R.N., Schmidt J., Mathur A., Stratton L., Kelly Y.F., Bird E., Waldron T., Liu E.C.-K., Zhang R., Lee H., Serafino R., Abboa-Offei B., Mathers P., Giancarli M., Seymour A.A., Webb M.L., Moreland S., Barrish J.C., Hunt J.T. Biphenylsulfonamide endothelin antagonists: structure-activity relationships of a series of mono- and disubstituted analogues and pharmacology of the orally active endothelin antagonist 2'-Amino-N-(3,4-dimethyl-5-isoxazolyl)-4'-(2-methylpropyl)[1,1'-biphenyl ]-2-sulfonamide (BMS-187308). J. Med. Chem. 1998, 41:5198-5218.
-
(1998)
J. Med. Chem.
, vol.41
, pp. 5198-5218
-
-
Murugesan, N.1
Gu, Z.2
Stein, P.D.3
Bisaha, S.4
Spergel, S.5
Girotra, R.6
Lee, V.G.7
Lloyd, J.8
Misra, R.N.9
Schmidt, J.10
Mathur, A.11
Stratton, L.12
Kelly, Y.F.13
Bird, E.14
Waldron, T.15
Liu, E.C.-K.16
Zhang, R.17
Lee, H.18
Serafino, R.19
Abboa-Offei, B.20
Mathers, P.21
Giancarli, M.22
Seymour, A.A.23
Webb, M.L.24
Moreland, S.25
Barrish, J.C.26
Hunt, J.T.27
more..
-
55
-
-
0034632777
-
A antagonists
-
A antagonists. J. Med. Chem. 2000, 43:3111-3117.
-
(2000)
J. Med. Chem.
, vol.43
, pp. 3111-3117
-
-
Murugesan, N.1
Gu, Z.2
Stein, P.D.3
Spergel, S.4
Mathur, A.5
Leith, L.6
Liu, E.C.-K.7
Zhang, R.8
Bird, E.9
Waldron, T.10
Marino, A.11
Morrison, R.A.12
Webb, M.L.13
Moreland, S.14
Barrish, J.C.15
-
56
-
-
18244406845
-
Biphenylsulfonamide endothelin receptor antagonists. Part 3: Structure-activity relationship of 4'-heterocyclic biphenylsulfonamides
-
Murugesan N., Gu Z., Stein P.D., Spergel S., Bisaha S., Liu E.C.-K., Zhang R., Webb M.L., Moreland S., Barrish J.C. Biphenylsulfonamide endothelin receptor antagonists. Part 3: Structure-activity relationship of 4'-heterocyclic biphenylsulfonamides. Bioorg. Med. Chem. Lett. 2002, 22:517-520.
-
(2002)
Bioorg. Med. Chem. Lett.
, vol.22
, pp. 517-520
-
-
Murugesan, N.1
Gu, Z.2
Stein, P.D.3
Spergel, S.4
Bisaha, S.5
Liu, E.C.-K.6
Zhang, R.7
Webb, M.L.8
Moreland, S.9
Barrish, J.C.10
-
57
-
-
0037413530
-
A selective antagonist
-
A 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
Humphreys, 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..
-
58
-
-
0000693239
-
The discovery of nonpeptide endothelin receptor antagonists. Progression towards bosentan
-
Neidhart W., Breu V., Bur D., Burri K., Clozel M., Hirth G., Mueller M., Wessel H.P., Ramuz H. The discovery of nonpeptide endothelin receptor antagonists. Progression towards bosentan. Chimia 1996, 50:519-524.
-
(1996)
Chimia
, vol.50
, pp. 519-524
-
-
Neidhart, W.1
Breu, V.2
Bur, D.3
Burri, K.4
Clozel, M.5
Hirth, G.6
Mueller, M.7
Wessel, H.P.8
Ramuz, H.9
-
59
-
-
84882502026
-
-
US 3,317,536 (May 2 1967 to Hoffmann La Roche)
-
Grussner, A., Lorch, E., Schnider, O. 4-Benzenesulfamidopyrimidines. US 3,317,536 (May 2 1967 to Hoffmann La Roche).
-
4-Benzenesulfamidopyrimidines
-
-
Grussner, A.1
Lorch, E.2
Schnider, O.3
-
60
-
-
0029896933
-
Discovery and optimization of a novel class of orally active nonpeptidic Endothelin-A receptor antagonists
-
Riechers H., Albrecht H.-P., Aberg W., Baumann E., Bernard H., Bohm H.-J., Klinge D., Kling A., Muller S., Raschack M., Unger L., Walker N., Wernet W. Discovery and optimization of a novel class of orally active nonpeptidic Endothelin-A receptor antagonists. J. Med. Chem. 1996, 39:2123-2128.
-
(1996)
J. Med. Chem.
, vol.39
, pp. 2123-2128
-
-
Riechers, H.1
Albrecht, H.-P.2
Aberg, W.3
Baumann, E.4
Bernard, H.5
Bohm, H.-J.6
Klinge, D.7
Kling, A.8
Muller, S.9
Raschack, M.10
Unger, L.11
Walker, N.12
Wernet, W.13
-
61
-
-
0036401042
-
Design and discovery of small molecules targeting Raf-1 kinase
-
Lowinger T.B., Riedl B., Dumas J., Smith R.A. Design and discovery of small molecules targeting Raf-1 kinase. Curr. Pharmaceut. Des. 2002, 8:2269-2278.
-
(2002)
Curr. Pharmaceut. Des.
, vol.8
, pp. 2269-2278
-
-
Lowinger, T.B.1
Riedl, B.2
Dumas, J.3
Smith, R.A.4
-
62
-
-
0033813234
-
Discovery of a new class of p38 kinase inhibitors
-
Dumas J., Sibley R., Riedl B., Monahan M.K., Lee W., Lowinger T.B., Redman A.M., Johnson J.S., Kingery-Wood J., Scott W.J., Smith R.A., Bobko M., Schoenleber R., Ranges G.E., Housley T.J., Bhargava A., Wilhelm S.M., Shrikhande A. Discovery of a new class of p38 kinase inhibitors. Bioorg. Med. Chem. Lett. 2000, 10:2047-2050.
-
(2000)
Bioorg. Med. Chem. Lett.
, vol.10
, pp. 2047-2050
-
-
Dumas, J.1
Sibley, R.2
Riedl, B.3
Monahan, M.K.4
Lee, W.5
Lowinger, T.B.6
Redman, A.M.7
Johnson, J.S.8
Kingery-Wood, J.9
Scott, W.J.10
Smith, R.A.11
Bobko, M.12
Schoenleber, R.13
Ranges, G.E.14
Housley, T.J.15
Bhargava, A.16
Wilhelm, S.M.17
Shrikhande, A.18
-
63
-
-
0037019275
-
-
Regan J., Breitfelder S., Cirillo P., Gilmore T., Graham A.G., Hickey E., Klaus B., Madwed J., Moriak M., Moss N., Pargellis C., Pav S., Proto A., Swinamer A., Tong L., Torcellini A. J. Med. Chem. 2002, 45:2994-3008.
-
(2002)
J. Med. Chem.
, vol.45
, pp. 2994-3008
-
-
Regan, J.1
Breitfelder, S.2
Cirillo, P.3
Gilmore, T.4
Graham, A.G.5
Hickey, E.6
Klaus, B.7
Madwed, J.8
Moriak, M.9
Moss, N.10
Pargellis, C.11
Pav, S.12
Proto, A.13
Swinamer, A.14
Tong, L.15
Torcellini, A.16
-
64
-
-
33745298429
-
Rational design of inhibitors that bind to inactive kinase conformations
-
Liu Y., Gray N.S. Rational design of inhibitors that bind to inactive kinase conformations. Nat. Chem. Biol. 2006, 2:358-364.
-
(2006)
Nat. Chem. Biol.
, vol.2
, pp. 358-364
-
-
Liu, Y.1
Gray, N.S.2
-
65
-
-
12144289677
-
Mechanism of activation of the RAF-ERK signaling pathway by oncogenic mutations of B-RAF
-
Cancer Genome Project
-
Wan P.T.C., Garnett M.J., Roe S.M., Lee S., Niculescu-Duvaz D., Good V.M., Jones M.C., Marshall C.J., Springer C.J., Barford D., Marais R. Mechanism of activation of the RAF-ERK signaling pathway by oncogenic mutations of B-RAF. Cell 2004, 116:855-867. Cancer Genome Project.
-
(2004)
Cell
, vol.116
, pp. 855-867
-
-
Wan, P.T.C.1
Garnett, M.J.2
Roe, S.M.3
Lee, S.4
Niculescu-Duvaz, D.5
Good, V.M.6
Jones, M.C.7
Marshall, C.J.8
Springer, C.J.9
Barford, D.10
Marais, R.11
-
66
-
-
33646751327
-
Evolution of the thienopyridine class of inhibitors of I kappa;B kinase beta: Part I: Hit-to-Lead strategies
-
Morwick T., Berry A., Brickwood J., Cardozo M., Catron K., DeTuri M., Emeigh J., Homon C., Hrapchak M., Jacober S., Jakes S., Kaplita P., Kelly T.A., Ksiazek J., Liuzzi M., Magolda R., Mao C., Marshall M., McNeil D., Prokopowicz A., Sarko C., Scouten E., Sledziona C., Sun S., Watrous J., Wu J.P., Cywin C.L. Evolution of the thienopyridine class of inhibitors of IκB kinase beta: Part I: Hit-to-Lead strategies. J. Med. Chem. 2006, 49:2898-2908.
-
(2006)
J. Med. Chem.
, vol.49
, pp. 2898-2908
-
-
Morwick, T.1
Berry, A.2
Brickwood, J.3
Cardozo, M.4
Catron, K.5
DeTuri, M.6
Emeigh, J.7
Homon, C.8
Hrapchak, M.9
Jacober, S.10
Jakes, S.11
Kaplita, P.12
Kelly, T.A.13
Ksiazek, J.14
Liuzzi, M.15
Magolda, R.16
Mao, C.17
Marshall, M.18
McNeil, D.19
Prokopowicz, A.20
Sarko, C.21
Scouten, E.22
Sledziona, C.23
Sun, S.24
Watrous, J.25
Wu, J.P.26
Cywin, C.L.27
more..
-
67
-
-
84882483890
-
-
Preparation of thiophenecarboxamides as inhibitors of the enzyme IKK-2 WO2001058890 (Astrazeneca)
-
Baxter, A., Brough, S., Faull, A., Johnstone, C., Mcinally, T. Preparation of thiophenecarboxamides as inhibitors of the enzyme IKK-2 WO2001058890 (Astrazeneca).
-
-
-
Baxter, A.1
Brough, S.2
Faull, A.3
Johnstone, C.4
Mcinally, T.5
-
68
-
-
84882517370
-
-
Preparation of aminothiophenes as NF-KB inhibitors. WO2003029242 (2003 Smithkline Beecham Corporation, USA). Parrish, C.A., Callahan, J.F., Wan, Z., Burgess, J. L., Stavenger, R. A., Holt, D. A. Preparation of 3-ureidothiophenes as angiogenesis and Chk1 kinase inhibitors for treating various forms of cancer and hyperproliferative disorders. WO2003028731 (Smithkline Beecham Corporation)
-
Wan, Z., Burgess, J. L., Callahan, J. F. Preparation of aminothiophenes as NF-KB inhibitors. WO2003029242 (2003 Smithkline Beecham Corporation, USA). Parrish, C.A., Callahan, J.F., Wan, Z., Burgess, J. L., Stavenger, R. A., Holt, D. A. Preparation of 3-ureidothiophenes as angiogenesis and Chk1 kinase inhibitors for treating various forms of cancer and hyperproliferative disorders. WO2003028731 (Smithkline Beecham Corporation).
-
-
-
Wan, Z.1
Burgess, J.L.2
Callahan, J.F.3
-
69
-
-
0041355495
-
A selective IKK-2 inhibitor blocks NF-B-dependent gene expression in Interleukin-1-stimulated synovial fibroblasts
-
Kishore N., Sommers C., Mathialagan S., Guzova J., Yao M., Hauser S., Huynh K., Bonar S., Mielke C., Albee L., Weier R., Graneto M., Hanau C., Perry T., Tripp C.S. A selective IKK-2 inhibitor blocks NF-B-dependent gene expression in Interleukin-1-stimulated synovial fibroblasts. J. Biol. Chem. 2003, 278:32861-32871.
-
(2003)
J. Biol. Chem.
, vol.278
, pp. 32861-32871
-
-
Kishore, N.1
Sommers, C.2
Mathialagan, S.3
Guzova, J.4
Yao, M.5
Hauser, S.6
Huynh, K.7
Bonar, S.8
Mielke, C.9
Albee, L.10
Weier, R.11
Graneto, M.12
Hanau, C.13
Perry, T.14
Tripp, C.S.15
-
70
-
-
84882527719
-
-
Heteroaromatic carboxamide derivatives, particularly 3-aminothiophene-2-carboxamides, useful as protein kinase inhibitors, for the treatment of cancer, inflammation, and inflammation-related disorders. WO2003037886 (Pharmacia Corporation, USA)
-
Graneto, M., Hanau, C. E., Perry, T. D. Heteroaromatic carboxamide derivatives, particularly 3-aminothiophene-2-carboxamides, useful as protein kinase inhibitors, for the treatment of cancer, inflammation, and inflammation-related disorders. WO2003037886 (Pharmacia Corporation, USA).
-
-
-
Graneto, M.1
Hanau, C.E.2
Perry, T.D.3
-
71
-
-
84882498246
-
-
Preparation of substituted thiophene carboxamide compounds for the treatment of inflammation. (Pharmacia Corporation, USA). WO2004009582
-
Hagen, T. J., Weier, R. M., Xu, X., Houdek, S. C., Clare, M. Preparation of substituted thiophene carboxamide compounds for the treatment of inflammation. (Pharmacia Corporation, USA). WO2004009582.
-
-
-
Hagen, T.J.1
Weier, R.M.2
Xu, X.3
Houdek, S.C.4
Clare, M.5
-
72
-
-
0037124196
-
Drugs, leads, and drug-likeness: an analysis of some recently launched drugs
-
Proudfoot J.R. Drugs, leads, and drug-likeness: an analysis of some recently launched drugs. Bioorg. Med. Chem. Lett. 2002, 12:1647-1650.
-
(2002)
Bioorg. Med. Chem. Lett.
, vol.12
, pp. 1647-1650
-
-
Proudfoot, J.R.1
-
73
-
-
33748742351
-
High content screening moves to the front of the line
-
Haney S.A., LaPan P., Pan J., Zhang J. High content screening moves to the front of the line. Drug Discov. Today. 2006, 11:889-894.
-
(2006)
Drug Discov. Today.
, vol.11
, pp. 889-894
-
-
Haney, S.A.1
LaPan, P.2
Pan, J.3
Zhang, J.4
-
74
-
-
32444441360
-
Computational chemistry driven decision making in lead generation
-
Schnecke V., Bostrom J. Computational chemistry driven decision making in lead generation. Drug Discov. Today. 2006, 11:43.
-
(2006)
Drug Discov. Today.
, vol.11
, pp. 43
-
-
Schnecke, V.1
Bostrom, J.2
-
75
-
-
0025679303
-
Inhibition of HIV-1 replication by a nonnucleoside reverse transcriptase inhibitor
-
Merluzzi V.J., Hargrave K.D., Labadia M., Grozinger K., Skoog M., Wu J.C., Shih C.K., Eckner K., Hattox S., Adams J., Rosenthal A.S. Inhibition of HIV-1 replication by a nonnucleoside reverse transcriptase inhibitor. Science. 1990, 250:1411-1413.
-
(1990)
Science.
, vol.250
, pp. 1411-1413
-
-
Merluzzi, V.J.1
Hargrave, K.D.2
Labadia, M.3
Grozinger, K.4
Skoog, M.5
Wu, J.C.6
Shih, C.K.7
Eckner, K.8
Hattox, S.9
Adams, J.10
Rosenthal, A.S.11
-
76
-
-
0028273009
-
Discovery, synthesis, and bioactivity of bis(heteroaryl)piperazines. 1. A novel class of non-nucleoside HIV-1 reverse transcriptase inhibitors
-
Romero D.L., Morge R.A., Biles C., Berrios-Pena N., May P.D., Palmer J.R., Johnson P.D., Smith H.W., Busso M., Tan C.-K., Voorman R.L., Reusser F., Althaus I.W., Downey K.M., So A.G., Resnick L., Tarpley W.G., Aristoff P.A. Discovery, synthesis, and bioactivity of bis(heteroaryl)piperazines. 1. A novel class of non-nucleoside HIV-1 reverse transcriptase inhibitors. J. Med. Chem. 1994, 37:999-1014.
-
(1994)
J. Med. Chem.
, vol.37
, pp. 999-1014
-
-
Romero, D.L.1
Morge, R.A.2
Biles, C.3
Berrios-Pena, N.4
May, P.D.5
Palmer, J.R.6
Johnson, P.D.7
Smith, H.W.8
Busso, M.9
Tan, C.-K.10
Voorman, R.L.11
Reusser, F.12
Althaus, I.W.13
Downey, K.M.14
So, A.G.15
Resnick, L.16
Tarpley, W.G.17
Aristoff, P.A.18
-
77
-
-
0027930721
-
Synthesis of a series of 4-(arylethynyl)-6-chloro-4-cyclopropyl-3,4-dihydroquinazolin-2(1H)-ones as novel non-nucleoside HIV-1 reverse transcriptase inhibitors
-
Tucker T.J., Lyle T.A., Wiscount C.M., Britcher S.F., Young S.D., Sanders W.M., Lumma W.C., Goldman M.E., O'Brien J.A., Ball R.G., Homnick C.F., Schleif W.A., Emini E.A., Huff J.R., Anderson P.A. Synthesis of a series of 4-(arylethynyl)-6-chloro-4-cyclopropyl-3,4-dihydroquinazolin-2(1H)-ones as novel non-nucleoside HIV-1 reverse transcriptase inhibitors. J. Med. Chem. 1994, 37:2437-2444.
-
(1994)
J. Med. Chem.
, vol.37
, pp. 2437-2444
-
-
Tucker, T.J.1
Lyle, T.A.2
Wiscount, C.M.3
Britcher, S.F.4
Young, S.D.5
Sanders, W.M.6
Lumma, W.C.7
Goldman, M.E.8
O'Brien, J.A.9
Ball, R.G.10
Homnick, C.F.11
Schleif, W.A.12
Emini, E.A.13
Huff, J.R.14
Anderson, P.A.15
-
78
-
-
0027096411
-
Non-peptide fibrinogen receptor antagonists. 1. Discovery and design of exosite inhibitors
-
Hartman G.D., Egbertson M.S., Halczenko W., Laswell W.L., Duggan M.E., Smith R.L., Naylor A.M., Manno P.D., Lynch R.J., Zhang G., Chang C.T.-C., Gould R. Non-peptide fibrinogen receptor antagonists. 1. Discovery and design of exosite inhibitors. J. Med. Chem. 1992, 35:4640-4642.
-
(1992)
J. Med. Chem.
, vol.35
, pp. 4640-4642
-
-
Hartman, G.D.1
Egbertson, M.S.2
Halczenko, W.3
Laswell, W.L.4
Duggan, M.E.5
Smith, R.L.6
Naylor, A.M.7
Manno, P.D.8
Lynch, R.J.9
Zhang, G.10
Chang, C.T.-C.11
Gould, R.12
-
79
-
-
0028106163
-
Epidermal growth factor receptor tyrosine kinase: investigation of catalytic mechanism, structure-based searching and discovery of a potent inhibitor
-
Ward W.H.J., Cook P.N., Slater A.M., Davies D.H., Holdgate G.A., Green L.R. Epidermal growth factor receptor tyrosine kinase: investigation of catalytic mechanism, structure-based searching and discovery of a potent inhibitor. Biochem. Pharmacol. 1994, 48:659-666.
-
(1994)
Biochem. Pharmacol.
, vol.48
, pp. 659-666
-
-
Ward, W.H.J.1
Cook, P.N.2
Slater, A.M.3
Davies, D.H.4
Holdgate, G.A.5
Green, L.R.6
-
80
-
-
0030454964
-
Non-peptidic inhibitors of human neutrophil elastase: the design and synthesis of sulfonanilide-containing inhibitors
-
Imaki K., Okada T., Nakayama Y., Nagao Y., Kobayashi K., Sakai Y., Mohri T., Amino T., Nakai H., Kawamura M. Non-peptidic inhibitors of human neutrophil elastase: the design and synthesis of sulfonanilide-containing inhibitors. Bioorg. Med. Chem. 1996, 4:2115-2134.
-
(1996)
Bioorg. Med. Chem.
, vol.4
, pp. 2115-2134
-
-
Imaki, K.1
Okada, T.2
Nakayama, Y.3
Nagao, Y.4
Kobayashi, K.5
Sakai, Y.6
Mohri, T.7
Amino, T.8
Nakai, H.9
Kawamura, M.10
-
81
-
-
0027959361
-
Acyclic NK1 antagonists: replacements for the benzhydryl group
-
Swain C.J., Cascieri M.A., Owens A., Saari W., Sadowski S., Strader C., Teall M., Van Niel M.B., Williams B.J. Acyclic NK1 antagonists: replacements for the benzhydryl group. Bioorg. Med. Chem. Lett. 1994, 4:2161-2164.
-
(1994)
Bioorg. Med. Chem. Lett.
, vol.4
, pp. 2161-2164
-
-
Swain, C.J.1
Cascieri, M.A.2
Owens, A.3
Saari, W.4
Sadowski, S.5
Strader, C.6
Teall, M.7
Van Niel, M.B.8
Williams, B.J.9
-
82
-
-
0032584086
-
Calcimimetics with potent and selective activity on the parathyroid calcium receptor
-
Nemeth E.F., Steffey M.E., Hammerland L.G., Hung B.C.P., Van Wagenen B.C., Delmar E.G., Balandrin M.F. Calcimimetics with potent and selective activity on the parathyroid calcium receptor. Proc. Natl. Acad. Sci. USA. 1998, 95:4040-4045.
-
(1998)
Proc. Natl. Acad. Sci. USA.
, vol.95
, pp. 4040-4045
-
-
Nemeth, E.F.1
Steffey, M.E.2
Hammerland, L.G.3
Hung, B.C.P.4
Van Wagenen, B.C.5
Delmar, E.G.6
Balandrin, M.F.7
-
83
-
-
0035935203
-
Discovery of heterocyclic ureas as a new class of raf kinase inhibitors: identification of a second generation lead by a combinatorial chemistry approach
-
Smith R.A., Barbosa J., Blum C.L., Bobko M.A., Caringal Y.V., Dally R., Johnson J.S., Katz M.E., Kennure N., Kingery-Wood J., Lee W., Lowinger T.B., Lyons J., Marsh V., Rogers D.H., Swartz S., Walling T., Wild H. Discovery of heterocyclic ureas as a new class of raf kinase inhibitors: identification of a second generation lead by a combinatorial chemistry approach. Bioorg. Med. Chem. Lett. 2001, 11:2775-2778.
-
(2001)
Bioorg. Med. Chem. Lett.
, vol.11
, pp. 2775-2778
-
-
Smith, R.A.1
Barbosa, J.2
Blum, C.L.3
Bobko, M.A.4
Caringal, Y.V.5
Dally, R.6
Johnson, J.S.7
Katz, M.E.8
Kennure, N.9
Kingery-Wood, J.10
Lee, W.11
Lowinger, T.B.12
Lyons, J.13
Marsh, V.14
Rogers, D.H.15
Swartz, S.16
Walling, T.17
Wild, H.18
-
84
-
-
0029621821
-
Structure-based design of sulfonamide-substituted non-peptidic HIV protease inhibitors
-
Skulnick H.I., Johnson P.D., Howe W.J., Tomich P.K., Chong K.-T., Watenpaugh K.D., Janakiraman M.N., Dolak L.A., McGrath J.P., Lynn J.C., Horng M.-M., Hinshaw R.R., Zipp G.L., Ruwart M.J., Schwende F.J., Zhong W.Z., Padbury G.E., Dalga R.J., Shiou L., Possert P.L., Rush B.D., Wilkinson K.F., Howard G.M., Toth L.N., Williams M.G., Kakuk T.J., Cole S.L., Zaya R.M., Lovasz K.D., Morris J.K., Romines K.R., Thaisrivongs S., Aristoff P.A. Structure-based design of sulfonamide-substituted non-peptidic HIV protease inhibitors. J. Med. Chem. 1995, 38:4968-4971.
-
(1995)
J. Med. Chem.
, vol.38
, pp. 4968-4971
-
-
Skulnick, H.I.1
Johnson, P.D.2
Howe, W.J.3
Tomich, P.K.4
Chong, K.-T.5
Watenpaugh, K.D.6
Janakiraman, M.N.7
Dolak, L.A.8
McGrath, J.P.9
Lynn, J.C.10
Horng, M.-M.11
Hinshaw, R.R.12
Zipp, G.L.13
Ruwart, M.J.14
Schwende, F.J.15
Zhong, W.Z.16
Padbury, G.E.17
Dalga, R.J.18
Shiou, L.19
Possert, P.L.20
Rush, B.D.21
Wilkinson, K.F.22
Howard, G.M.23
Toth, L.N.24
Williams, M.G.25
Kakuk, T.J.26
Cole, S.L.27
Zaya, R.M.28
Lovasz, K.D.29
Morris, J.K.30
Romines, K.R.31
Thaisrivongs, S.32
Aristoff, P.A.33
more..
-
85
-
-
0025797112
-
OPC-21268, an orally effective, nonpeptide vasopressin V1 receptor antagonist
-
Yamamura Y., Ogawa H., Chihara T., Kondo K., Onogawa T., Nakamura S., Mori T., Tominaga M., Yabuuchi Y. OPC-21268, an orally effective, nonpeptide vasopressin V1 receptor antagonist. Science 1991, 252:572-574.
-
(1991)
Science
, vol.252
, pp. 572-574
-
-
Yamamura, Y.1
Ogawa, H.2
Chihara, T.3
Kondo, K.4
Onogawa, T.5
Nakamura, S.6
Mori, T.7
Tominaga, M.8
Yabuuchi, Y.9
-
86
-
-
0033956395
-
Nonpeptide arginine vasopressin antagonists for both V1A and V2 receptors: synthesis and pharmacological properties of 4'-(1,4,5,6-tetrahydroimidazo[4,5-d][1]benzazepine-6-carbonyl)benzanilid e derivatives and 4'-(5,6-dihydro-4H-thiazolo[5,4-d][1]benzazepine-6-carbonyl)benzanilide derivative
-
Matsuhisa A., Taniguchi N., Koshio H., Yatsu T., Tanaka A. Nonpeptide arginine vasopressin antagonists for both V1A and V2 receptors: synthesis and pharmacological properties of 4'-(1,4,5,6-tetrahydroimidazo[4,5-d][1]benzazepine-6-carbonyl)benzanilid e derivatives and 4'-(5,6-dihydro-4H-thiazolo[5,4-d][1]benzazepine-6-carbonyl)benzanilide derivative. Chem. Pharmaceut. Bull. 2000, 48:21-31.
-
(2000)
Chem. Pharmaceut. Bull.
, vol.48
, pp. 21-31
-
-
Matsuhisa, A.1
Taniguchi, N.2
Koshio, H.3
Yatsu, T.4
Tanaka, A.5
-
87
-
-
0027185323
-
Orally active, nonpeptide vasopressin V1 antagonists. A novel series of 1-(1-substituted 4-piperidyl)-3,4-dihydro-2(1H)-quinolinones
-
Ogawa H., Yamamura Y., Miyamoto H., Kondo K., Yamashita H., Nakaya K., Chihara T., Mori T., Tominaga M., Yabuuchi Y. Orally active, nonpeptide vasopressin V1 antagonists. A novel series of 1-(1-substituted 4-piperidyl)-3,4-dihydro-2(1H)-quinolinones. J. Med. Chem. 1993, 36:2011-2017.
-
(1993)
J. Med. Chem.
, vol.36
, pp. 2011-2017
-
-
Ogawa, H.1
Yamamura, Y.2
Miyamoto, H.3
Kondo, K.4
Yamashita, H.5
Nakaya, K.6
Chihara, T.7
Mori, T.8
Tominaga, M.9
Yabuuchi, Y.10
-
88
-
-
0032474915
-
Synthesis and biological evaluations of 3-substituted indolin-2-ones: a novel class of tyrosine kinase inhibitors that exhibit selectivity toward particular receptor tyrosine kinases
-
Sun L., Tran N., Tang F., App H., Hirth P., McMahon G., Tang C. Synthesis and biological evaluations of 3-substituted indolin-2-ones: a novel class of tyrosine kinase inhibitors that exhibit selectivity toward particular receptor tyrosine kinases. J. Med. Chem. 1998, 41:2588-2603.
-
(1998)
J. Med. Chem.
, vol.41
, pp. 2588-2603
-
-
Sun, L.1
Tran, N.2
Tang, F.3
App, H.4
Hirth, P.5
McMahon, G.6
Tang, C.7
-
89
-
-
19944428353
-
Discovery of N-(2-chloro-6-methyl-phenyl)-2-(6-(4-(2-hydroxyethyl)-piperazin-1-yl)-2- methylpyrimidin-4-ylamino)thiazole-5-carboxamide (BMS-354825), a dual Src/Abl kinase inhibitor with potent antitumor activity in preclinical assays
-
Lombardo L.J., Lee F.Y., Chen P., Norris D., Barrish J.C., Behnia K., Castaneda S., Cornelius L.A.M., Das J., Doweyko A.M., Fairchild C., Hunt J.T., Inigo I., Johnston K., Kamath A., Kan D., Klei H., Marathe P., Pang S., Peterson R., Pitt S., Schieven G.L., Schmidt R.J., Tokarski J., Wen M.-L., Wityak J., Borzilleri R.M. Discovery of N-(2-chloro-6-methyl-phenyl)-2-(6-(4-(2-hydroxyethyl)-piperazin-1-yl)-2- methylpyrimidin-4-ylamino)thiazole-5-carboxamide (BMS-354825), a dual Src/Abl kinase inhibitor with potent antitumor activity in preclinical assays. J. Med. Chem. 2004, 47:6658-6661.
-
(2004)
J. Med. Chem.
, vol.47
, pp. 6658-6661
-
-
Lombardo, L.J.1
Lee, F.Y.2
Chen, P.3
Norris, D.4
Barrish, J.C.5
Behnia, K.6
Castaneda, S.7
Cornelius, L.A.M.8
Das, J.9
Doweyko, A.M.10
Fairchild, C.11
Hunt, J.T.12
Inigo, I.13
Johnston, K.14
Kamath, A.15
Kan, D.16
Klei, H.17
Marathe, P.18
Pang, S.19
Peterson, R.20
Pitt, S.21
Schieven, G.L.22
Schmidt, R.J.23
Tokarski, J.24
Wen, M.-L.25
Wityak, J.26
Borzilleri, R.M.27
more..
-
90
-
-
4544253908
-
Discovery of potent and selective beta;-homophenylalanine based dipeptidyl peptidase IV inhibitors
-
Xu J., Ok H.O., Gonzalez E.J., Colwell L.F., Jr, Habulihaz B., He H., Leiting B., Lyons K.A., Marsilio F., Patel R.A., Wu J.K., Thornberry N.A., Weber A.E., Parmee E.R. Discovery of potent and selective β-homophenylalanine based dipeptidyl peptidase IV inhibitors. Bioorg. Med. Chem. Lett. 2004, 14:4759-4762.
-
(2004)
Bioorg. Med. Chem. Lett.
, vol.14
, pp. 4759-4762
-
-
Xu, J.1
Ok, H.O.2
Gonzalez, E.J.3
Colwell Jr., L.F.4
Habulihaz, B.5
He, H.6
Leiting, B.7
Lyons, K.A.8
Marsilio, F.9
Patel, R.A.10
Wu, J.K.11
Thornberry, N.A.12
Weber, A.E.13
Parmee, E.R.14
-
91
-
-
27744548649
-
The discovery of the CCR5 receptor antagonist, UK-427,857, a new agent for the treatment of HIV infection and AIDS
-
Wood A., Armour D. The discovery of the CCR5 receptor antagonist, UK-427,857, a new agent for the treatment of HIV infection and AIDS. Progr. Med. Chem. 2005, 43:239-271.
-
(2005)
Progr. Med. Chem.
, vol.43
, pp. 239-271
-
-
Wood, A.1
Armour, D.2
|