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1
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0035513630
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Comprehensive survey of combinatorial library synthesis: 2000
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Dolle RE: Comprehensive survey of combinatorial library synthesis: 2000. J Combinatorial Chem (2001) 3:477-517.
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(2001)
J Combinatorial Chem
, vol.3
, pp. 477-517
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Dolle, R.E.1
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3
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0034684780
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2A antagonist
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2A antagonist. Bioorg Med Chem Lett (2000) 10:2693-2696. This paper illustrates the use of organometallic chemistry in the construction of a library of pharmacologically relevant compounds, which in turn has yielded novel, potent and selective lead material at a GPCR.
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(2000)
Bioorg Med Chem Lett
, vol.10
, pp. 2693-2696
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Smith, A.L.1
Stevenson, G.I.2
Lewis, S.3
Patel, S.4
Castro, J.L.5
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4
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18244382828
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Combinatorial synthesis of 3-(amidoalkyl) and 3-(aminoalkyl)-2-arylindole derivatives: Discovery of potent ligands for a variety of G-protein coupled receptors
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Willoughby CA, Hutchins SM, Rosauer KG, Dhar MJ, Chapman KT, Chicchi GG, Sadowski S, Weinberg DH, Patel S, Malkowitz L, Di Salvo J, Pacholok SG, 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. An interesting example of how library design based upon pharmacologically well-precedented structures can provide a rich variety of leads within a receptor superfamily. This paper also demonstrates the use of synthesis in mixtures in order to rapidly prepare large numbers of analogs.
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(2002)
Bioorg Med Chem Lett
, vol.12
, pp. 93-96
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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
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5
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0035921058
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Thrombin receptor (PAR-1) antagonists. Solid-phase synthesis of indole-based peptide mimetics by anchoring to a secondary amide
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Zhang H-C, McComsey DF, White KB, Addo MF, Andrade-Gordon P, Derian CK, Oksenberg D, Maryanoff BE: Thrombin receptor (PAR-1) antagonists. Solid-phase synthesis of indole-based peptide mimetics by anchoring to a secondary amide. Bioorg Med Chem Lett (2001) 11:2105-2109.
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(2001)
Bioorg Med Chem Lett
, vol.11
, pp. 2105-2109
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Zhang, H.-C.1
McComsey, D.F.2
White, K.B.3
Addo, M.F.4
Andrade-Gordon, P.5
Derian, C.K.6
Oksenberg, D.7
Maryanoff, B.E.8
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7
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0035931355
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Solid-phase synthesis of cyclic alkoxyketones, inhibitors of the cysteine protease cathepsin K
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Fenwick AE, Garnier B, Gribble AD, Ife RJ, Rawlings AD, Witherington J: Solid-phase synthesis of cyclic alkoxyketones, inhibitors of the cysteine protease cathepsin K. Bioorg Med Chem Lett (2001) 11:195-198. An example of the use of IRORI technology to allow discrete, single compounds to be synthesised using the efficient 'mix-and-split' solid-phase synthesis technique.
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(2001)
Bioorg Med Chem Lett
, vol.11
, pp. 195-198
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Fenwick, A.E.1
Garnier, B.2
Gribble, A.D.3
Ife, R.J.4
Rawlings, A.D.5
Witherington, J.6
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8
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0035921097
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Amino acid derived sulphonamide hydroxamates as inhibitors of procollagen C-proteinase: Solid-phase synthesis of ornithine analogues
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Dankwart SM, Martin RL, Chan CS, Van Wart HE, Walker KAM, Delaet NG, Robinson LA: Amino acid derived sulphonamide hydroxamates as inhibitors of procollagen C-proteinase: Solid-phase synthesis of ornithine analogues. Bioorg Med Chem Lett (2001) 11:2085-2088.
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(2001)
Bioorg Med Chem Lett
, vol.11
, pp. 2085-2088
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Dankwart, S.M.1
Martin, R.L.2
Chan, C.S.3
Van Wart, H.E.4
Walker, K.A.M.5
Delaet, N.G.6
Robinson, L.A.7
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9
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0034658164
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Solid-phase parallel synthesis of azarene pyrrolidinones as factor Xa inhibitors
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Gong Y, Becker M, Choi-Sledeski YM, Davis RS, Salvino JM, Chu V, Brown KD, Pauls HW: Solid-phase parallel synthesis of azarene pyrrolidinones as factor Xa inhibitors. Bioorg Med Chem Lett (2000) 10:1033-1036.
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(2000)
Bioorg Med Chem Lett
, vol.10
, pp. 1033-1036
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Gong, Y.1
Becker, M.2
Choi-Sledeski, Y.M.3
Davis, R.S.4
Salvino, J.M.5
Chu, V.6
Brown, K.D.7
Pauls, H.W.8
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10
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0035931468
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Solid-phase optimisation of achiral amidinobenzyl indoles as potent and selective factor Xa inhibitors
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Heinelt U, Herok S, Matter H, Wildgoose P: Solid-phase optimisation of achiral amidinobenzyl indoles as potent and selective factor Xa inhibitors. Bioorg Med Chem Lett (2001) 11:227-230. This paper provides an interesting example of the solid-phase synthesis to rapidly optimize the pharmacokinetic profile of an existing lead.
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(2001)
Bioorg Med Chem Lett
, vol.11
, pp. 227-230
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Heinelt, U.1
Herok, S.2
Matter, H.3
Wildgoose, P.4
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11
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0035854304
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Solid-phase synthesis of peptidomimetic inhibitors for the hepatitis C virus NS3 protease
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Poupart M-A, Cameron DR, Chabot C, Ghiro E, Goudreau N, Goulet S, Poirier M, Tsantrizos YS: Solid-phase synthesis of peptidomimetic inhibitors for the hepatitis C virus NS3 protease. J Org Chem (2001) 66:4743-4751.
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(2001)
J Org Chem
, vol.66
, pp. 4743-4751
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Poupart, M.-A.1
Cameron, D.R.2
Chabot, C.3
Ghiro, E.4
Goudreau, N.5
Goulet, S.6
Poirier, M.7
Tsantrizos, Y.S.8
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12
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0035829149
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Solid-phase synthesis of a library constructed of aromatic phosphate, long alkyl chains and tryptophane components, and identification of potent dipeptide telomerase inhibitors
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Sasaki S, Ehara T, Alam MR, Fujino Y, Harada N, Kimura J, Nakamura H, Maeda M: Solid-phase synthesis of a library constructed of aromatic phosphate, long alkyl chains and tryptophane components, and identification of potent dipeptide telomerase inhibitors. Bioorg Med Chem Lett (2001) 11:2581-2584.
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(2001)
Bioorg Med Chem Lett
, vol.11
, pp. 2581-2584
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Sasaki, S.1
Ehara, T.2
Alam, M.R.3
Fujino, Y.4
Harada, N.5
Kimura, J.6
Nakamura, H.7
Maeda, M.8
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13
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0035821594
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Solid-phase synthesis of a nonpeptide RGD mimetic library: New selective αvβ3 integrin antagonists
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Sulyok GAG, Gibson C, Goodman SL, Holzemann G, Wiesner M, Kessler H: Solid-phase synthesis of a nonpeptide RGD mimetic library: New selective αvβ3 integrin antagonists. J Med Chem (2001) 44:1938-1950.
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(2001)
J Med Chem
, vol.44
, pp. 1938-1950
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Sulyok, G.A.G.1
Gibson, C.2
Goodman, S.L.3
Holzemann, G.4
Wiesner, M.5
Kessler, H.6
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15
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0034219844
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Solid-phase synthesis of tetrasubstituted pyrazoles, novel ligands for the estrogen receptor
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Stauffer SR, Katzenellenbogen JA: Solid-phase synthesis of tetrasubstituted pyrazoles, novel ligands for the estrogen receptor. J Combinatorial Chem (2000) 2:318-329. Results suggest that certain tetrasubstituted pyrazoles have high affinity and potency as agonists and antagonists for the estrogen α-subtype receptor.
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(2000)
J Combinatorial Chem
, vol.2
, pp. 318-329
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Stauffer, S.R.1
Katzenellenbogen, J.A.2
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16
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0035921072
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Parallel solid-phase synthesis of nucleoside phosphoramidate libraries
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Jin Y, Chen X, Côté M-E, Roland A, Korba B, Mounir S, Iyer RP: Parallel solid-phase synthesis of nucleoside phosphoramidate libraries. Bioorg Med Chem Lett (2001) 11:2057-2060.
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(2001)
Bioorg Med Chem Lett
, vol.11
, pp. 2057-2060
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Jin, Y.1
Chen, X.2
Côté, M.-E.3
Roland, A.4
Korba, B.5
Mounir, S.6
Iyer, R.P.7
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17
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0035817222
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Discovery and SAR of org 24598 - A selective glycine uptake inhibitor
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Brown A, Carlyle I, Clark J, Hamilton W, Gibson S, McGarry G, McEachen S, Rae D, Thom S, Walker G: Discovery and SAR of org 24598 - a selective glycine uptake inhibitor. Bioorg Med Chem Lett (2001) 11:2007-2009.
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(2001)
Bioorg Med Chem Lett
, vol.11
, pp. 2007-2009
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Brown, A.1
Carlyle, I.2
Clark, J.3
Hamilton, W.4
Gibson, S.5
McGarry, G.6
McEachen, S.7
Rae, D.8
Thom, S.9
Walker, G.10
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18
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3543056384
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Solid- and solution-phase synthesis of vancomycin and vancomycin analogues with activity against vancomycin-resistant bacteria
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Nicolaou KC, Cho SY, Hughes R, Winssinger N, Smethurst C, Labischinski H, Endermann R: Solid- and solution-phase synthesis of vancomycin and vancomycin analogues with activity against vancomycin-resistant bacteria. Chem Eur J (2001) 7:3798-3823. Results suggest that vancomycin derivatives, modified on one of the sugar residues, provide highly potent antibacterial agents effective against vancomycin-resistant bacteria.
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(2001)
Chem Eur J
, vol.7
, pp. 3798-3823
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Nicolaou, K.C.1
Cho, S.Y.2
Hughes, R.3
Winssinger, N.4
Smethurst, C.5
Labischinski, H.6
Endermann, R.7
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19
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0035900319
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The development and application of a novel safety-catch linker for BOC-based assembly of libraries of cyclic peptides
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Boume GT, Golding SW, McGeary RP, Meutermans WDF, Jones A, Marshall GR, Alewood PF, Smythe ML: The development and application of a novel safety-catch linker for BOC-based assembly of libraries of cyclic peptides. J Org Chem (2001) 66:7706-7713. Results indicate that through development of novel solid-phase strategies, large arrays of cyclic peptides can now be accessed.
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(2001)
J Org Chem
, vol.66
, pp. 7706-7713
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Boume, G.T.1
Golding, S.W.2
McGeary, R.P.3
Meutermans, W.D.F.4
Jones, A.5
Marshall, G.R.6
Alewood, P.F.7
Smythe, M.L.8
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20
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0035909633
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Traceless solid-phase synthesis of 1,2,4-triazoles using a novel amine resin
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Larsen SD, DiPaolo BA: Traceless solid-phase synthesis of 1,2,4-triazoles using a novel amine resin. Org Lett (2001) 3:3341-3344. Results indicate that the development of a novel solid-phase linker allows access to medicinally relevant 1,2,4-triazoles where two points of diversity have been introduced.
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(2001)
Org Lett
, vol.3
, pp. 3341-3344
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Larsen, S.D.1
DiPaolo, B.A.2
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21
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0035907472
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Regio-reactive resin: A platform for orthogonal loading using the polymer backbone and cross-linker
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Dickerson TJ, Reed NN, Janda KD: Regio-reactive resin: A platform for orthogonal loading using the polymer backbone and cross-linker. Bioorg Med Chem Lett (2001) 11:1507-1509.
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(2001)
Bioorg Med Chem Lett
, vol.11
, pp. 1507-1509
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Dickerson, T.J.1
Reed, N.N.2
Janda, K.D.3
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