Abstract
A series of four bicyclic cores were prepared and evaluated as cyclin-dependent kinase-2 (CDK2) inhibitors. From the in-vitro and cell-based analysis, the pyrazolo[1,5-a]pyrimidine core (represented by 9) emerged as the superior core for further elaboration in the identification of novel CDK2 inhibitors.
MeSH terms
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Binding Sites
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Crystallography, X-Ray
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Cyclin-Dependent Kinase 2 / chemistry
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Cyclin-Dependent Kinase 2 / drug effects*
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Cyclin-Dependent Kinase Inhibitor Proteins / chemical synthesis
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Cyclin-Dependent Kinase Inhibitor Proteins / chemistry*
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Cyclin-Dependent Kinase Inhibitor Proteins / pharmacology*
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Drug Design
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Inhibitory Concentration 50
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Molecular Structure
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Protein Binding
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Protein Kinase Inhibitors / chemical synthesis
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Protein Kinase Inhibitors / chemistry*
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Protein Kinase Inhibitors / pharmacology*
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Pyrazoles / chemical synthesis
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Pyrazoles / chemistry*
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Pyrazoles / pharmacology*
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Pyrimidines / chemical synthesis
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Pyrimidines / chemistry*
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Pyrimidines / pharmacology*
Substances
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Cyclin-Dependent Kinase Inhibitor Proteins
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Protein Kinase Inhibitors
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Pyrazoles
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Pyrimidines
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pyrazolo(1,5-a)pyrimidine
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Cyclin-Dependent Kinase 2