Non-oxime pyrazole based inhibitors of B-Raf kinase

…, N Littman, M Callejo, M Martinson, S Galbraith…

Index: Newhouse, Bradley J.; Hansen, Joshua D.; Grina, Jonas; Welch, Mike; Topalov, George; Littman, Nicole; Callejo, Michele; Martinson, Matthew; Galbraith, Sarah; Laird, Ellen R.; Brandhuber, Barbara J.; Vigers, Guy; Morales, Tony; Woessner, Rich; Randolph, Nikole; Lyssikatos, Joseph; Olivero, Alan Bioorganic and Medicinal Chemistry Letters, 2011 , vol. 21, # 11 p. 3488 - 3492

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Citation Number: 22

Abstract

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.