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

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

  • Bioorg Med Chem Lett. 2013 Aug 1;23(15):4381-7. doi: 10.1016/j.bmcl.2013.05.074.
Arno G Steinig 1,  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,  Ryan Schulz,  Andy Cooke,  Mark Bittner,  Roy W Turton,  Maryland Franklin,  Prafulla Gokhale,  Darla Landfair,  Christine Mantis,  Jen Workman,  Robert Wild,  Jonathan Pachter,  David Epstein,  Mark J Mulvihill
Affiliations

Affiliation

  • 1 OSI Pharmaceuticals, LLC, A Wholly-Owned Subsidiary of Astellas US, 1 Bioscience Park Drive, Farmingdale, NY 11735, USA. [email protected]
PMID: 23773865 DOI: 10.1016/j.bmcl.2013.05.074
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.

Figures
Products
  • Cat. No.
    Product Name
    Description
    Target
    Research Area
  • HY-118269
    cMET/RON kinases Inhibitor