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

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.

Graphical abstractCompounds belonging to several scaffolds—quinazolines, quinolines and quinoxalines—were designed and synthesized as Raf kinase inhibitors. Scaffolds were assessed for invitro BrafV600E inhibit ion, and overall kina se selectivity. Pharmacokinetic parameters for one of the scaffolds were also determined.Figure optionsDownload full-size imageDownload as PowerPoint slide