Pyrido[2,3-d]pyrimidin-7-one Inhibitors of Cyclin-Dependent Kinases

M Barvian, DH Boschelli, J Cossrow… - Journal of medicinal …, 2000 - ACS Publications
The identification of 8-ethyl-2-phenylamino-8 H-pyrido [2, 3-d] pyrimidin-7-one (1) as an
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 …

Pyrido[2,3-d]pyrimidin-7-one Inhi-bitors of Cyclin-Dependent Kinases.

M Barvian, DH Boschelli, J Cossrow… - Journal of Medicinal …, 2001 - ACS Publications
… Carbonic Anhydrase and Matrix Metalloproteinase Inhibitors: Sulfonylated Amino Acid
Hydroxamates with MMP Inhibitory Properties Act as Efficient Inhibitors of CA Isozymes I, II,
and IV, and N-Hydroxysulfonamides Inhibit Both These Zinc Enzymes … Table 2 is missing
compounds 71r80; thus the data are included below. … e CA inhibition (but not MMP and
ChC inhibition) data from ref 42. …
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