1256962-77-2Relevant academic research and scientific papers
4-(pyrazol-4-yl)-pyrimidines as selective inhibitors of cyclin-dependent kinase 4/6
Cho, Young Shin,Borland, Maria,Brain, Christopher,Chen, Christine H.-T.,Cheng, Hong,Chopra, Rajiv,Chung, Kristy,Groarke, James,He, Guo,Hou, Ying,Kim, Sunkyu,Kovats, Steven,Lu, Yipin,O'Reilly, Marc,Shen, Junqing,Smith, Troy,Trakshel, Gary,V?gtle, Markus,Xu, Mei,Xu, Ming,Sung, Moo Je
, p. 7938 - 7957 (2011/03/19)
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.
