Acyl Dipeptides as reversible caspase inhibitors. Part 2: Further optimization

被引:19
作者
Linton, SD
Karanewsky, DS
Ternansky, RJ
Chen, N
Guo, M
Jahangiri, KG
Kalish, VJ
Meduna, SP
Robinson, ED
Ullman, BR
Wu, JC
Pham, B
Kodandapani, L
Smidt, R
Diaz, JL
Fritz, LC
von Krosigk, U
Roggo, S
Schmitz, A
Tomaselli, KJ
机构
[1] Idun Pharmaceut Inc, San Diego, CA 92121 USA
[2] Novartis Pharma Ltd, Pharma Res, CH-4002 Basel, Switzerland
关键词
D O I
10.1016/S0960-894X(02)00630-3
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
A new structural class of broad spectrum caspase inhibitors was optimized for its activity against caspases 1, 3, 6, 7, and 8. The most potent compound had low nanomolar broad spectrum activity, in particular, single digit nanomolar inhibitory activity against caspase 8. (C) 2002 Elsevier Science Ltd. All rights reserved.
引用
收藏
页码:2973 / 2975
页数:3
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