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

  title={Potent and selective pyrazole-based inhibitors of B-Raf kinase.},
  author={Joshua D Hansen and Jonas A. Grina and Brad Newhouse and Mike Welch and George Topalov and Nicole Littman and Michele Callejo and Susan L. Gloor and Matthew Martinson and Ellen R. Laird and Barbara J. Brandhuber and Guy P. A. Vigers and Tony H Morales and Rich Woessner and Nikole Randolph and Joseph P. Lyssikatos and Alan G. Olivero},
  journal={Bioorganic & medicinal chemistry letters},
  volume={18 16},
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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