Novel 6-aminofuro [3, 2-c] pyridines as potent, orally efficacious inhibitors of cMET and RON kinases

…, PA Tavares-Greco, T Wang, MR Albertella…

文献索引：Steinig, Arno G.; Li, An-Hu; Wang, Jing; Chen, Xin; Dong, Hanqing; Ferraro, Caterina; Jin, Meizhong; Kadalbajoo, Mridula; Kleinberg, Andrew; Stolz, Kathryn M.; Tavares-Greco, Paula A.; Wang, Ti; Albertella, Mark R.; Peng, Yue; Crew, Linda; Kahler, Jennifer; Kan, Julie; Schulz, Ryan; Cooke, Andy; Bittner, Mark; Turton, Roy W.; Franklin, Maryland; Gokhale, Prafulla; Landfair, Darla; Mantis, Christine; Workman, Jen; Wild, Robert; Pachter, Jonathan; Epstein, David; Mulvihill, Mark J. Bioorganic and Medicinal Chemistry Letters, 2013 , vol. 23, # 15 p. 4381 - 4387

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被引用次数: 10

摘要

A series of novel 6-aminofuro [3, 2-c] pyridines as kinase inhibitors is described, most notably, OSI-296 (6). We discuss our exploration of structure–activity relationships and optimization leading to OSI-296 and disclose its pharmacological activity against cMET and RON in cellular assays. OSI-296 is a potent and selective inhibitor of cMET and RON kinases that shows in vivo efficacy in tumor xenografts models upon oral dosing and is ...