Synthesis of aminopyrazole analogs and their evaluation as CDK inhibitors for cancer therapy

Bioorganic & Medicinal Chemistry Letters
2018.0

Abstract

We synthesized a library of aminopyrazole analogs to systematically explore the hydrophobic pocket adjacent to the hinge region and the solvent exposed region of cyclin dependent kinases. Structure-activity relationship studies identified an optimal substitution for the hydrophobic pocket and analog 24 as a potent and selective CDK2/5 inhibitor.

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