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Synthesis and structure activity relationships of a series of 4-amino-1H-pyrazoles as covalent inhibitors of CDK14.

ABSTRACT: The TAIRE family of kinases are an understudied branch of the CDK kinase family, that have been implicated in a number of cancers. This manuscript describes the design, synthesis and SAR of covalent CDK14 inhibitors, culminating in identification of FMF-04-159-2, a potent, covalent CDK14 inhibitor with a TAIRE kinase biased selectivity profile.

SUBMITTER: Ferguson FM

PROVIDER: S-EPMC6886737 | biostudies-literature | 2019 Aug

REPOSITORIES: biostudies-literature

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Synthesis and structure activity relationships of a series of 4-amino-1H-pyrazoles as covalent inhibitors of CDK14.

Ferguson Fleur M FM Doctor Zainab M ZM Ficarro Scott B SB Marto Jarrod A JA Kim Nam Doo ND Sim Taebo T Gray Nathanael S NS

Bioorganic & medicinal chemistry letters 20190523 15

The TAIRE family of kinases are an understudied branch of the CDK kinase family, that have been implicated in a number of cancers. This manuscript describes the design, synthesis and SAR of covalent CDK14 inhibitors, culminating in identification of FMF-04-159-2, a potent, covalent CDK14 inhibitor with a TAIRE kinase biased selectivity profile. ...[more]

PMID: 31175010

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