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ID: ALA1136528

Journal: Bioorg Med Chem Lett

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

Authors: Li X, Huang P, Cui JJ, Zhang J, Tang C.

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 novel series of pyrrolyllactone and pyrrolyllactam indolinones as potent CDK2 inhibitors.

CiteXplore: 12749903

DOI: 10.1016/s0960-894x(03)00312-3