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Design and synthesis of 6, 6-fused heterocyclic amides as raf kinase inhibitors

S Ramurthy, A Costales, JM Jansen, B Levine…

文献索引:Ramurthy, Savithri; Costales, Abran; Jansen, Johanna M.; Levine, Barry; Renhowe, Paul A.; Shafer, Cynthia M.; Subramanian, Sharadha Bioorganic and Medicinal Chemistry Letters, 2012 , vol. 22, # 4 p. 1678 - 1681

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被引用次数: 12

摘要

Compounds belonging to several scaffolds—quinazolines, quinolines and quinoxalines— were designed and synthesized as Raf kinase inhibitors. Scaffolds were assessed for in vitro BrafV600E inhibition, and overall kinase selectivity. Pharmacokinetic parameters for one of the scaffolds were also determined.