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  • Title: Potent and selective pyrazole-based inhibitors of B-Raf kinase.
    Author: Hansen JD, Grina J, Newhouse B, Welch M, Topalov G, Littman N, Callejo M, Gloor S, Martinson M, Laird E, Brandhuber BJ, Vigers G, Morales T, Woessner R, Randolph N, Lyssikatos J, Olivero A.
    Journal: Bioorg Med Chem Lett; 2008 Aug 15; 18(16):4692-5. PubMed ID: 18676143.
    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.
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