Development of potent B-RafV600E inhibitors containing an arylsulfonamide headgroup
John C Stellwagen1, George M Adjabeng, Marc R Arnone
1GlaxoSmithKline Oncology CEDD, Research Triangle Park, NC 27709-3398, United States. john.stellwagen@amgen.com
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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