Abstract
Using a high-throughput screening campaign, we identified the 4,6-bis anilino pyrimidines as inhibitors of the cyclin-dependent kinase, CDK4. Herein we describe the further chemical modification and use of X-ray crystallography to develop potent and selective in vitro inhibitors of CDK4.
MeSH terms
-
Animals
-
Antineoplastic Agents / chemical synthesis
-
Antineoplastic Agents / pharmacology*
-
Binding Sites
-
Crystallography, X-Ray
-
Cyclin-Dependent Kinase 4
-
Cyclin-Dependent Kinases / antagonists & inhibitors*
-
Humans
-
Inhibitory Concentration 50
-
Molecular Structure
-
Proto-Oncogene Proteins*
-
Pyrimidines / chemical synthesis
-
Pyrimidines / pharmacology*
-
Structure-Activity Relationship
Substances
-
Antineoplastic Agents
-
Proto-Oncogene Proteins
-
Pyrimidines
-
CDK4 protein, human
-
Cyclin-Dependent Kinase 4
-
Cyclin-Dependent Kinases