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Synthesis and biological evaluation of quinoxaline derivatives as specific c-Met kinase inhibitors
Institution:1. Student Research Committee, Pharmaceutical Sciences Research Center, Department of Medicinal Chemistry, Mazandaran University of Medical Sciences, Sari, Iran;2. Pharmaceutical Sciences Research Center, Department of Medicinal Chemistry, Mazandaran University of Medical Sciences, Sari, Iran;3. Molecular and Cell Biology Research Center, Hemoglobinopathy Institute, Faculty of Medicine, Mazandaran University of Medical Sciences, Sari, Iran;4. Department of Medicinal Chemistry, School of Pharmacy, Ardabil University of Medical Sciences, Ardabil, Iran
Abstract:A series of novel quinoxaline derivatives were synthesized and evaluated for their inhibitory activity against c-Met kinase enzyme. Most of the tested compounds exhibited potent inhibitory activity. All the synthesized quinoxaline compounds were further examined against c-Met overexpressed human gastric cancer cell line (MKN-45), which showed good inhibitory activity. Among the synthesized compounds, compound 4 exhibited better tumor growth inhibition in the animal model study; we also confirmed its acceptable drug property and highly selective target activity.
Keywords:Quinoxaline  c-Met inhibitors  c-Met kinase  Synthesis
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