Abstract
Quinazolines have been identified as inhibitors of CDK4/D1 and CDK2/E. Aspects of the SAR were investigated using solution-phase, parallel synthesis. An X-ray crystal structure was obtained of quinazoline 51 bound in CDK2 and key interactions within the ATP binding pocket are defined.
MeSH terms
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Binding, Competitive / drug effects
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Cell Line
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Crystallography, X-Ray
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Cyclin-Dependent Kinases / antagonists & inhibitors*
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Enzyme Inhibitors / chemical synthesis*
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Enzyme Inhibitors / pharmacology
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Models, Molecular
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Quinazolines / chemical synthesis*
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Structure-Activity Relationship
Substances
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Enzyme Inhibitors
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Quinazolines
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Cyclin-Dependent Kinases