Synthesis and CHK1 inhibitory potency of Hymenialdisine analogues

被引：31
|
作者：
Parmentier, Jean-Gilles [1 ]
Portevin, Bernard [1 ]
Golsteyn, Roy M. [2 ]
Pierre, Alain [2 ]
Hickman, John [2 ]
Gloanec, Philippe [1 ]
De Nanteuil, Guillaume [1 ]
机构：
[1] Inst Rech Servier, Med Chem Div D, F-92150 Suresnes, France
[2] Inst Rech Servier, Div Cancerol, F-78290 Croissy Sur Seine, France
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2009年 / 19卷 / 03期
关键词：
Hymenialdisine; CHK1; inhibitor; CHECKPOINT; KINASES;
D O I：
10.1016/j.bmcl.2008.12.001
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
A series of thieno[3,2-b]pyrroloazepinones derivatives related to Hymenialdisine were prepared and tested for CHK1 inhibitory activity. Nanomolar inhibitions were achieved when electron-withdrawing substituents were introduced at position 3 of the thiophene ring. (C) 2008 Elsevier Ltd. All rights reserved.
引用
收藏
页码：841 / 844
页数：4
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