Potent inhibition of checkpoint kinase activity by a hymenialdisine-derived indoloazepine

被引：67

作者：

Sharma, V ^{[1
]}

Tepe, JJ ^{[1
]}

机构：

[1] Michigan State Univ, Dept Chem, E Lansing, MI 48824 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2004年 / 14卷 / 16期

关键词：

hymenialdisine; kinase; checkpoint; Chk2; apoptosis;

D O I：

10.1016/j.bmcl.2004.05.079

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The marine sponge metabolite hymenialdisine is a potent inhibitor of a variety of kinases including MEK-1, GSK-3beta, and CK1. In addition, hymenialdisine and debromohymenialdisine exhibit inhibition of the G(2) cell cycle checkpoint at micromolar concentrations. We report herein the potent inhibition of cell cycle kinase Chk(2) by the indolic-hymenialdisine indoloazepine 1 (IC50 = 8 nM). (C) 2004 Elsevier Ltd. All rights reserved.

引用

页码：4319 / 4321

页数：3

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