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  • Development of potent B-Raf...
    Stellwagen, John C; Adjabeng, George M; Arnone, Marc R; Dickerson, Scott H; Han, Chao; Hornberger, Keith R; King, Alastair J; Mook, Robert A; Petrov, Kimberly G; Rheault, Tara R; Rominger, Cynthia M; Rossanese, Olivia W; Smitheman, Kimberly N; Waterson, Alex G; Uehling, David E

    Bioorganic & medicinal chemistry letters, 08/2011, Letnik: 21, Številka: 15
    Journal Article

    A potent series of inhibitors against the B-Raf super(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.)