Abstract
A novel series of anilinopyrazoles has been designed based on the X-ray crystal structure analysis. Most compounds from this series not only show sub-nanomolar IC(50) values for CDK2, but also demonstrate almost 1000-fold selectivity to other kinases including CDK1.
MeSH terms
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Binding Sites
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CDC2-CDC28 Kinases / antagonists & inhibitors*
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CDC2-CDC28 Kinases / chemistry
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Crystallography, X-Ray*
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Cyclin-Dependent Kinase 2
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Drug Design
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Enzyme Inhibitors / chemical synthesis
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Enzyme Inhibitors / pharmacology
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Humans
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Inhibitory Concentration 50
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Models, Molecular
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Protein Binding
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Pyrazoles / chemical synthesis*
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Pyrazoles / pharmacology
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Structure-Activity Relationship
Substances
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Enzyme Inhibitors
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Pyrazoles
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CDC2-CDC28 Kinases
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CDK2 protein, human
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Cyclin-Dependent Kinase 2