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

doi:10.1016/j.bmcl.2013.05.074

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Article

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

Bioorganic & medicinal chemistry letters - 1 Aug 2013

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

Abstract excerpt

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...

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PMID: 23773865
DOI: 10.1016/j.bmcl.2013.05.074

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