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    Bioorg Med Chem Lett. 2008 Aug 15;18(16):4692-5. Epub 2008 Jul 5.

    Potent and selective pyrazole-based inhibitors of B-Raf kinase.

    Source

    Lead Optimization, Array BioPharma, 3200 Walnut Street, Boulder, CO 80301, USA. josh.hansen@arraybiopharma.com

    Abstract

    Herein we describe a novel pyrazole-based class of ATP competitive B-Raf inhibitors. These inhibitors exhibit both excellent cellular potency and striking B-Raf selectivity. A subset of these inhibitors has demonstrated the ability to inhibit downstream ERK phosphorylation in LOX tumors from mouse xenograft studies.

    PMID:
    18676143
    [PubMed - indexed for MEDLINE]

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