Novel pyrazinone mono-amides as potent and reversible caspase-3 inhibitors

被引：32
作者：
Han, YX
Giroux, A
Colucci, J
Bayly, CI
Mckay, DJ
Roy, S
Xanthoudakis, S
Vaillancourt, J
Rasper, DM
Tam, J
Tawa, P
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 Frosst Ctr Therapeut Res, Dept Biochem & Mol Biol, Pointe Claire, PQ H9R 4P8, Canada
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2005年 / 15卷 / 04期
关键词：
pyrazinone mono-amide; caspase-3; inhibitors;
D O I：
10.1016/j.bmcl.2004.12.006
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
The iterative process for the discovery of a series of pyrazinone mono-amides as potent, selective and reversible non-peptide caspase-3 inhibitors (e.g., M826 and M867) is reported. These compounds display potent anti apoptotic activities in a number of cell based systems in vitro as well as in several animal models in vivo. (C) 2004 Elsevier Ltd. All rights reserved.
引用
收藏
页码：1173 / 1180
页数：8
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