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Development of potent B-RafV600E inhibitors containing an arylsulfonamide headgroup |
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| Authors: | 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 |
| Affiliation: | a GlaxoSmithKline Oncology CEDD, Five Moore Drive, Research Triangle Park, NC 27709-3398, United States b GlaxoSmithKline Oncology CEDD, 1250 South Collegeville Road, Collegeville, PA 19426-0989, United States |
| Abstract: | A potent series of inhibitors against the B-RafV600E 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. |
| Keywords: | B-RafV600E Sulfonamide Thiazole |
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