Design,synthesis and biological evaluation of type-II VEGFR-2 inhibitors based on quinoxaline scaffold |
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| Institution: | 1. Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Hacettepe University, Ankara, Turkey;2. Drug Design and Discovery Lab, Zewail City of Science and Technology, Cairo 12578, Egypt;3. Biomedical Sciences Program, University of Science and Technology, Zewail City of Science and Technology, Cairo 12578, Egypt;1. Pharmaceutical Medicinal Chemistry & Drug Design Department, Faculty of Pharmacy (Boys), Al-Azhar University, Cairo 11884, Egypt;2. Pharmaceutical Chemistry Department, Faculty of Pharmacy, Heliopolis University for Sustainable Development, Cairo, Egypt;3. Zoology Department, Faculty of Science, Al-Azhar University, Cairo 11884, Egypt;4. Pharmacognosy Department, Faculty of Pharmacy (Boys), Al-Azhar University, Cairo 11884, Egypt;5. Department of Agriculture Chemistry, Faculty of Agriculture, Damietta University, Damietta, Egypt;6. National Center for Natural Products Research, University of Mississippi, MS 38677, USA;7. Department of Pharmacognosy, Faculty of Pharmacy, Alexandria University, Alexandria, Egypt;8. Department of Pharmaceutics and Drug Delivery, University of Mississippi, University, MS 38677, USA;9. Pharmaceutical Organic Chemistry Department, Faculty of Pharmacy, Al-Azhar University, Nasr City, 11884 Cairo, Egypt;10. Pharmaceutical Chemistry Department, Faculty of Pharmacy, Horus University – Egypt, International Costal Road, New Damietta, Egypt;1. Pharmaceutical Chemistry Department, Faculty of Pharmacy, Al-Azhar University, Cairo, Egypt;2. Pharmaceutical Chemistry Department, Faculty of Pharmacy, Heliopolis University for Sustainable Development, Cairo, Egypt;3. MD in Clinical Pathology, Blood Bank Specialist, Blood Bank Directorate Manager, Ministry of Health, Cairo, Egypt |
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| Abstract: | In an effort to develop ATP-competitive VEGFR-2 selective inhibitors, a series of new quinoxaline-based derivatives was designed and synthesized. The target compounds were biologically evaluated for their inhibitory activity against VEGFR-2. The design of the target compounds was accomplished after a profound study of the structure activity relationship (SAR) of type-II VEGFR-2 inhibitors. Among the synthesized compounds, 1-(2-((4-methoxyphenyl)amino)-3-oxo-3,4 dihydroquinoxalin-6-yl)-3-phenylurea (VIIa) displayed the highest inhibitory activity against VEGFR-2. Molecular modeling study involving molecular docking and field alignment was implemented to interpret the variable inhibitory activity of the newly synthesized compounds. |
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| Keywords: | VEGFR-2 Kinase Type-II Quinoxaline Docking study |
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