The discovery of potent and selective 4-aminothienopyridines as B-Raf kinase inhibitors |
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| Authors: | Jun Tang Karen E Lackey Scott H Dickerson |
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| Institution: | GlaxoSmithKline Research & Development, Research Triangle Park, NC 27709, USA |
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| Abstract: | A series of novel, potent 4-aminothienopyridine B-Raf kinase inhibitors was designed and synthesized using knowledge-based design. Compounds 5f, and 6k exhibited not only excellent potency in both enzyme assay (IC50 = 5.1, 16.6 nM) and cellular assay (IC50 = 0.2, 0.2 μM), but also had an outstanding selectivity profile against other kinases. |
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