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  • Title: Non-oxime pyrazole based inhibitors of B-Raf kinase.
    Author: Newhouse BJ, Hansen JD, Grina J, Welch M, Topalov G, Littman N, Callejo M, Martinson M, Galbraith S, Laird ER, Brandhuber BJ, Vigers G, Morales T, Woessner R, Randolph N, Lyssikatos J, Olivero A.
    Journal: Bioorg Med Chem Lett; 2011 Jun 01; 21(11):3488-92. PubMed ID: 21536432.
    Abstract:
    The synthesis and biological evaluation of non-oxime pyrazole based B-Raf inhibitors is reported. Several oxime replacements have been prepared and have shown excellent enzyme activity. Further optimization of fused pyrazole 2a led to compound 38, a selective and potent B-Raf inhibitor.
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