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. 2008 Aug 15;18(16):4692-5.
doi: 10.1016/j.bmcl.2008.07.002. Epub 2008 Jul 5.

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

Joshua D Hansen  1 , Jonas Grina, Brad Newhouse, Mike Welch, George Topalov, Nicole Littman, Michele Callejo, Susan Gloor, Matthew Martinson, Ellen Laird, Barbara J Brandhuber, Guy Vigers, Tony Morales, Rich Woessner, Nikole Randolph, Joseph Lyssikatos, Alan Olivero
Affiliations

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

Joshua D Hansen et al. Bioorg Med Chem Lett. .

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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