AI Article Synopsis
- A new series of compounds called 6-aminofuro[3,2-c]pyridines, particularly OSI-296, are developed as kinase inhibitors.
- The study highlights the structure-activity relationships and optimization processes that led to the creation of OSI-296, focusing on its effectiveness against cMET and RON.
- OSI-296 is proven to be a strong and selective inhibitor of cMET and RON kinases, demonstrating effective tumor suppression in animal models after oral administration with good tolerance.
Article 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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| http://dx.doi.org/10.1016/j.bmcl.2013.05.074 | DOI Listing |
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