Synthesis and structure-activity relationships of a novel series of pyrimidines as potent inhibitors of TBK1/IKKε kinases

Edward G. McIver, Justin Bryans, Kristian Birchall, Jasveen Chugh, Thomas Drake, Stephen J. Lewis, Joanne Osborne, Ela Smiljanic-Hurley, William Tsang, Ahmad Kamal, Alison Levy, Michelle Newman, Debra Taylor, J. Simon C. Arthur, Kristopher Clark, Philip Cohen

    Research output: Contribution to journalArticlepeer-review

    26 Citations (Scopus)

    Abstract

    The design, synthesis and structure-activity relationships of a novel series of 2,4-diamino-5-cyclopropyl pyrimidines is described. Starting from BX795, originally reported to be a potent inhibitor of PDK1, we have developed compounds with improved selectivity and drug-like properties. These compounds have been evaluated in a range of cellular and in vivo assays, enabling us to probe the putative role of the TBK1/IKKe pathway in inflammatory diseases.

    Original languageEnglish
    Pages (from-to)7169-7173
    Number of pages5
    JournalBioorganic & Medicinal Chemistry Letters
    Volume22
    Issue number23
    DOIs
    Publication statusPublished - Dec 2012

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