Discovery of novel aspartyl ketone dipeptides as potent and selective caspase-3 inhibitors

被引：30

作者：

Han, YX

Giroux, A

Grimm, EL

Aspiotis, R

Francoeur, S

Bayly, CI

Mckay, DJ

Roy, S

Xanthoudakis, S

Vaillancourt, JP

Rasper, DM

Tam, J

Tawa, P

Thornberry, NA

Paterson, EP

Garcia-Calvo, M

Becker, JW

Rotonda, J

Nicholson, DW

Zamboni, RJ

机构：

[1] Merck Frosst Canada Inc, Merck Frosst Ctr Therapeut Res, Dept Med Chem, Pointe Claire, PQ H9R 4P8, Canada

[2] Merck Frosst Canada Inc, Merck Ctr Therapeut Res, Dept Biochem & Mol Biol, Quebec City, PQ H9R 4P8, Canada

[3] Merck & Co Inc, Merck Res Labs, Dept Enzymol, Rahway, NJ 07065 USA

[4] Merck & Co Inc, Merck Res Labs, Dept Biol Struct, Rahway, NJ 07065 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2004年 / 14卷 / 03期

关键词：

D O I：

10.1016/j.bmcl.2003.10.064

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The discovery of a series of potent, selective and reversible dipeptidyl caspase-3 inhibitors are reported. The iterative discovery process of using combinatorial chemistry, parallel synthesis, moleculare modelling and structural biology will be discussed. (C) 2003 Elsevier Ltd. All rights reserved.

引用

页码：805 / 808

页数：4

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BECKER JW, UNPUB J MED CHEM

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