Development of potent B-RafV600E inhibitors containing an arylsulfonamide headgroup

  • Bioorg Med Chem Lett. 2011 Aug 1;21(15):4436-40. doi: 10.1016/j.bmcl.2011.06.021.
John C Stellwagen  1 ,  George M Adjabeng ,  Marc R Arnone ,  Scott H Dickerson ,  Chao Han ,  Keith R Hornberger ,  Alastair J King ,  Robert A Mook Jr ,  Kimberly G Petrov ,  Tara R Rheault ,  Cynthia M Rominger ,  Olivia W Rossanese ,  Kimberly N Smitheman ,  Alex G Waterson ,  David E Uehling
Affiliations
  • 1. GlaxoSmithKline Oncology CEDD, Research Triangle Park, NC 27709-3398, United States. [email protected]
PMID: 21733693 DOI: 10.1016/j.bmcl.2011.06.021
Abstract

A potent series of inhibitors against the B-Raf(V600E) kinase have been developed that show excellent activity in cellular assays and good oral bioavailability in rats. The key structural features of the series are an arylsulfonamide headgroup, a thiazole core, and a fluorine ortho to the sulfonamide nitrogen.

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