The identification, synthesis, protein crystal structure and in vitro biochemical evaluation of a new 3,4-diarylpyrazole class of Hsp90 inhibitors

Kwai-Ming J. Cheung, Thomas P. Matthews, Karen Ball, Martin Rowlands, Kathy Boxall, Swee Sharp, Alison Maloney, S. Mark Roe, Chrisostomos Prodromou, Laurence Pearl, Wynne Aherne, Edward MacDonald, Paul Workman

    Research output: Contribution to journalArticlepeer-review

    Abstract

    High-throughput screening identified the 3,4-diarylpyrazole CCT018159 as a novel and potent (7.1 μM) inhibitor of Hsp90 ATPase activity. Here, we describe the synthesis of CCT018159 and a number of close analogues together with data on their biochemical properties. Some initial structure–activity relationships are discussed, as well as the crystal structure of CCT018159 bound to Hsp90.
    Original languageEnglish
    Pages (from-to)3338-3343
    JournalBioorganic & Medicinal Chemistry Letters
    Volume15
    Issue number14
    DOIs
    Publication statusPublished - 15 Jul 2005

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