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