inhibitor of Cdk4 led to the initiation of a program to evaluate related pyrido [2, 3-d] pyrimidin-
7-ones for inhibition of cyclin-dependent kinases (Cdks). Analysis of more than 60
analogues has identified some clear SAR trends that may be exploited in the design of more
potent Cdk inhibitors. The most potent Cdk4 inhibitors reported in this study inhibit Cdk4 with
IC50= 0.004 μM ([ATP]= 25 μM). X-ray crystallographic analysis of representative …