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.

journal_name

Bioorg Med Chem Lett

authors

Ferguson FM,Doctor ZM,Ficarro SB,Marto JA,Kim ND,Sim T,Gray NS

doi

10.1016/j.bmcl.2019.05.024

subject

Has Abstract

pub_date

2019-08-01 00:00:00

pages

1985-1993

issue

15

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(19)30321-X

journal_volume

29

pub_type

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