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

X Li, P Huang, JJ Cui, J Zhang, C Tang

Index: Li, Xiaoyuan; Huang, Ping; Cui, Jingrong Jean; Zhang, Jennifer; Tang, Cho Bioorganic and Medicinal Chemistry Letters, 2003 , vol. 13, # 11 p. 1939 - 1942

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Citation Number: 33

Abstract

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 ...

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