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4-(Pyrazol-4-yl)-pyrimidines as Selective Inhibitors of Cyclin-Dependent Kinase 4/6

Cho, Young and Borland, Maria and Brain, Christopher and Chen, Christine and Cheng, Hong and Chopra, Rajiv and Chung, Kristy and Groarke, James and He, Guo and Hou, Ying and Kovats, Steven and Shen, Junqing and Trakshel, Gary and Voegtle, Markus and Xu, Mei and Xu, Ming and Sung, Moo (2010) 4-(Pyrazol-4-yl)-pyrimidines as Selective Inhibitors of Cyclin-Dependent Kinase 4/6. Journal of Medicinal Chemistry, 53 (22). pp. 7938-7957. ISSN 0022-2623

Abstract

Identification and structure-guided optimization of a series of 4-(pyrazol-4-yl)-pyrimidines as selective CDK4/6 inhibitors is reported herein. Several potency and selectivity determinants were established based on the X-ray crystallographic analysis of representative compounds bound to monomeric CDK6. Significant selectivity for CDK4/6 over CDK1 and CDK2 was demonstrated with several compounds in both enzymatic and cellular assays.

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Date Deposited: 13 Oct 2015 13:16
Last Modified: 13 Oct 2015 13:16
URI: https://oak.novartis.com/id/eprint/2806

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