Substituted aminobenzimidazole pyrimidines as cyclin-dependent kinase inhibitors

被引：20
|
作者：
Verma, S
Nagarathnam, D
Shao, JX
Zhang, L
Zhao, J
Wang, YM
Li, TD
Mull, E
Enyedy, I
Wang, CG
Zhu, QM
Altieri, M
Jordan, J
Dang, TTA
Reddy, S
机构：
[1] Bayer Res Ctr, Dept Chem Res, West Haven, CT 06516 USA
[2] Bayer Res Ctr, Dept Canc Res, West Haven, CT 06516 USA
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2005年 / 15卷 / 08期
关键词：
D O I：
10.1016/j.bmcl.2005.02.076
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
A series of aminobenzimidazole-substituted pyrimidines were synthesized and evaluated for biochemical activity against CDK1. A high-speed parallel synthesis approach enabled the identification of a potent lead series having improved potency in the CDK1 assay (IC50 < 10 nM). Cell cycle analysis showed that the compounds induced a G2/M block. Docking studies were carried out with a CDK1 homology model, and provide a rationale for the observed activities. (c) 2005 Elsevier Ltd. All rights reserved.
引用
收藏
页码：1973 / 1977
页数：5
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