Abstract
High-throughput screening identified the imidazo[1,2-a]pyridine and bisanilinopyrimidine series as inhibitors of the cyclin-dependent kinase CDK4. Comparison of their experimentally-determined binding modes and emerging structure-activity trends led to the development of potent and selective imidazo[1,2-a]pyridine inhibitors for CDK4 and in particular CDK2.
MeSH terms
-
CDC2-CDC28 Kinases / antagonists & inhibitors
-
CDC2-CDC28 Kinases / chemistry
-
Crystallography, X-Ray
-
Cyclin-Dependent Kinase 2
-
Cyclin-Dependent Kinase 4
-
Cyclin-Dependent Kinases / antagonists & inhibitors*
-
Cyclin-Dependent Kinases / chemistry
-
Enzyme Inhibitors / chemical synthesis
-
Enzyme Inhibitors / chemistry
-
Enzyme Inhibitors / pharmacology
-
Humans
-
Inhibitory Concentration 50
-
Molecular Structure
-
Protein Binding
-
Proto-Oncogene Proteins*
-
Pyridines / chemical synthesis*
-
Pyridines / chemistry
-
Pyridines / pharmacology
-
Structure-Activity Relationship
Substances
-
Enzyme Inhibitors
-
Proto-Oncogene Proteins
-
Pyridines
-
CDC2-CDC28 Kinases
-
CDK2 protein, human
-
CDK4 protein, human
-
Cyclin-Dependent Kinase 2
-
Cyclin-Dependent Kinase 4
-
Cyclin-Dependent Kinases