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


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.

SUBMITTER: Rana S 

PROVIDER: S-EPMC6295223 | biostudies-literature | 2018 Dec

REPOSITORIES: biostudies-literature