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

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

Index: 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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Citation Number: 12

Abstract

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.