Synthesis and biological evaluation of novel pazopanib derivatives as antitumor agents |
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| Institution: | 1. Department of Chemistry and Physics, Florida Gulf Coast University, Fort Myers, Florida 33965, United States;2. Department of Chemistry, University of South Alabama, Mobile, Alabama 36688, United States;3. Department of Chemistry and Biochemistry, University of Texas at Arlington, Arlington, Texas 76019, United States;4. Department of Chemistry, Umeå University, SE-901 87 Umeå, Sweden |
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| Abstract: | A series of novel pazopanib derivatives, 7a–m, were designed and synthesized by modification of terminal benzene and indazole rings in pazopanib. The structures of all the synthesized compounds were confirmed by 1H NMR and MS. Their inhibitory activity against VEGFR-2, PDGFR-α and c-kit tyrosine kinases were evaluated. All the compounds exhibited definite kinase inhibition, in which compound 7l was most potent with IC50 values of 12 nM against VEGFR-2. Furthermore, compounds 7c, 7d and 7m demonstrated comparable inhibitory activity against three tyrosine kinases to pazopanib, and compound 7f showed superior inhibitory effects than that of pazopanib. |
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| Keywords: | Pazopanib derivatives Synthesis Tyrosine kinase Inhibitory activity |
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