Abstract
Through chemical modification and X-ray crystallography we identified the 2,4-bis anilino pyrimidines as potent inhibitors of CDK4. Herein, we describe the optimisation of this series.
MeSH terms
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Adenosine Triphosphate / chemistry
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Animals
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Antineoplastic Agents / chemical synthesis
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Antineoplastic Agents / pharmacology*
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Binding Sites
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Crystallography, X-Ray
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Cyclin-Dependent Kinase 4
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Cyclin-Dependent Kinases / antagonists & inhibitors*
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Humans
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Inhibitory Concentration 50
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Molecular Structure
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Proto-Oncogene Proteins*
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Pyrimidines / chemical synthesis
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Pyrimidines / pharmacology*
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Structure-Activity Relationship
Substances
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Antineoplastic Agents
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Proto-Oncogene Proteins
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Pyrimidines
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Adenosine Triphosphate
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CDK4 protein, human
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Cyclin-Dependent Kinase 4
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Cyclin-Dependent Kinases