Synthesis and structure activity relationships of a series of 4-amino-1H-pyrazoles as covalent inhibitors of CDK14. Issue 15 (1st August 2019)

• Record Type: Journal Article
• Authors: Ferguson, Fleur M.; Doctor, Zainab M.; Ficarro, Scott B.; Marto, Jarrod A.; Kim, Nam Doo; Sim, Taebo; Gray, Nathanael S.
• Is Part Of: Bioorganic & medicinal chemistry letters. Volume 29:Issue 15(2019)
• Page Start: 1985
• Page End: 1993
• Publication Date: 2019-08-01
• Subjects: Covalent kinase inhibitor -- CDK14 -- TAIRE kinase -- CDK15 -- CDK16 -- CDK17 -- CDK18 -- CDK inhibitor -- Mitosis -- Cell cycle; Bioorganic chemistry -- Periodicals; Pharmaceutical chemistry -- Periodicals; 572
• DOI: 10.1016/j.bmcl.2019.05.024
• Languages: English
• ISSNs: 0960-894X

Abstract

Graphical abstract: 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.