4KNB

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

Steinig, A.G., Li, A.H., Wang, J., Chen, X., Dong, H., Ferraro, C., Jin, M., Kadalbajoo, M., Kleinberg, A., Stolz, K.M., Tavares-Greco, P.A., Wang, T., Albertella, M.R., Peng, Y., Crew, L., Kahler, J., Kan, J., Schulz, R., Cooke, A., Bittner, M., Turton, R.W., Franklin, M., Gokhale, P., Landfair, D., Mantis, C., Workman, J., Wild, R., Pachter, J., Epstein, D., Mulvihill, M.J.

(2013) Bioorg Med Chem Lett 23: 4381-4387

• PubMed: 23773865 Search on PubMed
• DOI: https://doi.org/10.1016/j.bmcl.2013.05.074
• Primary Citation of Related Structures:  
  4KNB


• PubMed 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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Organizational Affiliation: 

OSI Pharmaceuticals, LLC, A Wholly-Owned Subsidiary of Astellas US, 1 Bioscience Park Drive, Farmingdale, NY 11735, USA. arnosteinig@gmail.com