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Design and synthesis of 5,6-fused heterocyclic amides as Raf kinase inhibitors |
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| Authors: | Ramurthy Savithri Aikawa Mina Amiri Payman Costales Abran Hashash Ahmad Jansen Johanna M Lin Song Ma Sylvia Renhowe Paul A Shafer Cynthia M Subramanian Sharadha Sung Leonard Verhagen Joelle |
| Institution: | a Global Discovery Chemistry/Oncology and Exploratory Chemistry, Novartis Institutes for Biomedical Research, 4560 Horton Street, Emeryville, CA 94608, USA b Oncolog Research, Novartis Institutes for Biomedical Research, 4560 Horton Street, Emeryville, CA 94608, USA c Gilead, 333 Lakeside Drive, Foster City, CA 94404, USA |
| Abstract: | Two scaffolds based on 5,6-fused heterocyclic backbones were designed and synthesized as Raf kinase inhibitors. The scaffolds were assessed for in vitro pan-Raf inhibition, activity in cell proliferation and target modulation assays, and pharmacokinetic parameters. |
| Keywords: | MAPK ras-mitogen activated protein kinase VEGFR vascular endothelial growth factor receptor PDGFR platelet-derived growth factor receptor CSF-1 colony stimulating factor-1 receptor RTK&rsquo s receptor tyrosine kinases STK&rsquo s serine threonine kinases Lck Leukocyte specific protein tyrosine kinase |
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