Synthesis and Evaluation of Indenopyrazoles as Cyclin-Dependent Kinase Inhibitors. 3. Structure Activity Relationships at C3 1, 2

…, DA Nugiel, C Benware, PA Benfield…

Index: Yue, Eddy W.; Higley, C. Anne; DiMeo, Susan V.; Carini, David J.; Nugiel, David A.; Benware, Carrie; Benfield, Pamela A.; Burton, Catherine R.; Cox, Sarah; Grafstrom, Robert H.; Sharp, Diane M.; Sisk, Lisa M.; Boylan, John F.; Muckelbauer, Jodi K.; Smallwood, Angela M.; Chen, Haiying; Chang, Chong-Hwan; Seitz, Steven P.; Trainor, George L. Journal of Medicinal Chemistry, 2002 , vol. 45, # 24 p. 5233 - 5248

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Citation Number: 49

Abstract

The identification of indeno [1, 2-c] pyrazol-4-ones as inhibitors of cyclin-dependent kinases (CDKs) has led to the discovery of a series of novel and potent compounds. Herein, we report the effects of substitutions at C3 of the indeno [1, 2-c] pyrazol-4-one core with alkyls, heterocycles, and substituted phenyls. Substitutions at the para position of the phenyl ring at C3 were generally well-tolerated; however, larger groups were generally inactive. For ...