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ID: ALA1806396

Journal: Bioorg Med Chem Lett

Title: Development of potent B-RafV600E inhibitors containing an arylsulfonamide headgroup.

Authors: Stellwagen JC, Adjabeng GM, Arnone MR, Dickerson SH, Han C, Hornberger KR, King AJ, Mook RA, Petrov KG, Rheault TR, Rominger CM, Rossanese OW, Smitheman KN, Waterson AG, Uehling DE.

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.

CiteXplore: 21733693

DOI: 10.1016/j.bmcl.2011.06.021