Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
10593553 | Bioorganic & Medicinal Chemistry Letters | 2013 | 7 Pages |
Abstract
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.
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Authors
Arno G. Steinig, An-Hu Li, Jing Wang, Xin Chen, Hanqing Dong, Caterina Ferraro, Meizhong Jin, Mridula Kadalbajoo, Andrew Kleinberg, Kathryn M. Stolz, Paula A. Tavares-Greco, Ti Wang, Mark R. Albertella, Yue Peng, Linda Crew, Jennifer Kahler, Julie Kan,