Bioorganic & medicinal chemistry letters, 2013-08, Vol.23 (15), p.4381-4387
- 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.
2013
Volltextzugriff (PDF)
Details
- Autor(en) / Beteiligte
- 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.
- Titel
- Novel 6-aminofuro[3,2-c]pyridines as potent, orally efficacious inhibitors of cMET and RON kinases
- Ist Teil von
- Bioorganic & medicinal chemistry letters, 2013-08, Vol.23 (15), p.4381-4387
- Ort / Verlag
- England: Elsevier Ltd
- Erscheinungsjahr
- 2013
- Quelle
- ScienceDirect
- Beschreibungen/Notizen
- 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.
- Sprache
- Englisch
- Identifikatoren
- ISSN: 0960-894XeISSN: 1464-3405DOI: 10.1016/j.bmcl.2013.05.074Titel-ID: cdi_proquest_miscellaneous_1500787278
- Format
- –
- Schlagworte
- Animals, Antineoplastic Agents - chemistry, Antineoplastic Agents - pharmacokinetics, Antineoplastic Agents - therapeutic use, Cell Line, Tumor, Cell Survival - drug effects, cMET, Female, Furopyridines, Half-Life, Humans, Hydrogen-Ion Concentration, Mice, Mice, Nude, Mutation, Neoplasms - drug therapy, Phosphorylation - drug effects, phosphotransferases (kinases), Protein Kinase Inhibitors - chemistry, Protein Kinase Inhibitors - pharmacokinetics, Protein Kinase Inhibitors - therapeutic use, Proto-Oncogene Proteins c-met - antagonists & inhibitors, Proto-Oncogene Proteins c-met - genetics, Proto-Oncogene Proteins c-met - metabolism, pyridines, Pyridines - chemistry, Pyridines - pharmacokinetics, Pyridines - therapeutic use, Rats, Rats, Sprague-Dawley, Receptor Protein-Tyrosine Kinases - antagonists & inhibitors, Receptor Protein-Tyrosine Kinases - metabolism, RON, Structure-Activity Relationship, structure-activity relationships, Transplantation, Heterologous, Tumor growth inhibition, Tyrosine kinase inhibitor