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

Fleur M. Ferguson, Zainab M. Doctor, Scott B. Ficarro, Jarrod A. Marto, Nam Doo Kim, Taebo Sim, Nathanael S. Gray

    Research output: Contribution to journalArticlepeer-review

    3 Citations (Scopus)

    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.

    Original languageEnglish
    Pages (from-to)1985-1993
    Number of pages9
    JournalBioorganic and Medicinal Chemistry Letters
    Volume29
    Issue number15
    DOIs
    Publication statusPublished - 2019 Aug 1

    Bibliographical note

    Publisher Copyright:
    © 2019 Elsevier Ltd

    Keywords

    • CDK inhibitor
    • CDK14
    • CDK15
    • CDK16
    • CDK17
    • CDK18
    • Cell cycle
    • Covalent kinase inhibitor
    • Mitosis
    • TAIRE kinase

    ASJC Scopus subject areas

    • Biochemistry
    • Molecular Medicine
    • Molecular Biology
    • Pharmaceutical Science
    • Drug Discovery
    • Clinical Biochemistry
    • Organic Chemistry

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