1175300-08-9Relevant articles and documents
Novel 6-aminofuro[3,2-c]pyridines as potent, orally efficacious inhibitors of cMET and RON kinases
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.
, p. 4381 - 4387 (2013/07/26)
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 well tolerated.
