دورية أكاديمية
Novel 6-aminofuro[3,2-c]pyridines as potent, orally efficacious inhibitors of cMET and RON kinases.
| العنوان: | Novel 6-aminofuro[3,2-c]pyridines as potent, orally efficacious inhibitors of cMET and RON kinases. |
|---|---|
| المؤلفون: | Steinig AG; OSI Pharmaceuticals, LLC, A Wholly-Owned Subsidiary of Astellas US, 1 Bioscience Park Drive, Farmingdale, NY 11735, USA. arnosteinig@gmail.com, Li AH, Wang J, Chen X, Dong H, Ferraro C, Jin M, Kadalbajoo M, Kleinberg A, Stolz KM, Tavares-Greco PA, Wang T, Albertella MR, Peng Y, Crew L, Kahler J, Kan J, Schulz R, Cooke A, Bittner M, Turton RW, Franklin M, Gokhale P, Landfair D, Mantis C, Workman J, Wild R, Pachter J, Epstein D, Mulvihill MJ |
| المصدر: | Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2013 Aug 01; Vol. 23 (15), pp. 4381-7. Date of Electronic Publication: 2013 May 30. |
| نوع المنشور: | Journal Article |
| اللغة: | English |
| بيانات الدورية: | Publisher: Elsevier Science Ltd Country of Publication: England NLM ID: 9107377 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1464-3405 (Electronic) Linking ISSN: 0960894X NLM ISO Abbreviation: Bioorg Med Chem Lett Subsets: MEDLINE |
| أسماء مطبوعة: | Publication: Oxford : Elsevier Science Ltd Original Publication: Oxford ; New York : Pergamon Press, c1991- |
| مواضيع طبية MeSH: | Antineoplastic Agents/*chemistry , Protein Kinase Inhibitors/*chemistry , Proto-Oncogene Proteins c-met/*antagonists & inhibitors , Pyridines/*chemistry , Receptor Protein-Tyrosine Kinases/*antagonists & inhibitors, Animals ; Antineoplastic Agents/pharmacokinetics ; Antineoplastic Agents/therapeutic use ; Cell Line, Tumor ; Cell Survival/drug effects ; Female ; Half-Life ; Humans ; Hydrogen-Ion Concentration ; Mice ; Mice, Nude ; Mutation ; Neoplasms/drug therapy ; Phosphorylation/drug effects ; Protein Kinase Inhibitors/pharmacokinetics ; Protein Kinase Inhibitors/therapeutic use ; Proto-Oncogene Proteins c-met/genetics ; Proto-Oncogene Proteins c-met/metabolism ; Pyridines/pharmacokinetics ; Pyridines/therapeutic use ; Rats ; Rats, Sprague-Dawley ; Receptor Protein-Tyrosine Kinases/metabolism ; Structure-Activity Relationship ; Transplantation, Heterologous |
| مستخلص: | 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. (Copyright © 2013 Elsevier Ltd. All rights reserved.) |
| المشرفين على المادة: | 0 (Antineoplastic Agents) 0 (OSI-296) 0 (Protein Kinase Inhibitors) 0 (Pyridines) EC 2.7.10.1 (Proto-Oncogene Proteins c-met) EC 2.7.10.1 (RON protein) EC 2.7.10.1 (Receptor Protein-Tyrosine Kinases) |
| تواريخ الأحداث: | Date Created: 20130619 Date Completed: 20140124 Latest Revision: 20161125 |
| رمز التحديث: | 20231215 |
| DOI: | 10.1016/j.bmcl.2013.05.074 |
| PMID: | 23773865 |
| قاعدة البيانات: | MEDLINE |
Full Text Finder | تدمد: | 1464-3405 |
|---|---|
| DOI: | 10.1016/j.bmcl.2013.05.074 |