Novel pyrrolyllactone and pyrrolyllactam indolinones as potent cyclin-dependent kinase 2 inhibitors

被引：34

作者：

Li, XY ^{[1
]}

Huang, P ^{[1
]}

Cui, JJ ^{[1
]}

Zhang, J ^{[1
]}

Tang, C ^{[1
]}

机构：

[1] SUGEN Inc, San Francisco, CA 94080 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2003年 / 13卷 / 11期

关键词：

D O I：

10.1016/S0960-894X(03)00312-3

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Cyclin-dependent kinases (CDKs) are essential in the control of cell cycle progression. Inhibition of CDKs represents a new approach for pharmacological intervention in the treatment of a variety of proliferative diseases, especially cancer. Based on the crystal structure of CDK2 in complex with an imidazole indolinone compound 1 (SU9516), lead optimization through modeling, synthesis, and SAR studies has led to the discovery of a novel series of pyrrolyllactone and pyrrolyllactam indolinones as potent CDK2 inhibitors. (C) 2003 Elsevier Science Ltd. All rights reserved.

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页码：1939 / 1942

页数：4

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