4-(Pyrazol-4-yl)-pyrimidines as Selective Inhibitors of Cyclin-Dependent Kinase 4/6
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Cho, Young, Borland, Maria, Brain, Christopher, Chen, Christine, Cheng, Hong, Chopra, Rajiv, Chung, Kristy, Groarke, James, He, Guo, Hou, Ying, Kovats, Steven, Shen, Junqing, Trakshel, Gary, Voegtle, Markus, Xu, Mei, 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 |