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STELLWAGEN, John C; ADJABENG, George M; ROMINGER, Cynthia M; ROSSANESE, Olivia W; SMITHEMAN, Kimberly N; WATERSON, Alex G; UEHLING, David E; ARNONE, Marc R; DICKERSON, Scott H; CHAO HAN; HORNBERGER, Keith R; KING, Alastair J; MOOK, Robert A; PETROV, Kimberly G; RHEAULT, Tara R
Bioorganic & medicinal chemistry letters, 2011-Aug-01, Letnik: 21, Številka: 15Journal Article
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.
