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https://ir.swu.ac.th/jspui/handle/123456789/14481| Title: | Synthesis, in vitro evaluation, and docking studies of novel chromone derivatives as HIV-1 protease inhibitor |
| Authors: | Ungwitayatorn J. Wiwat C. Samee W. Nunthanavanit P. Phosrithong N. |
| Keywords: | Chromone derivatives Chromones Cyclization reactions HIV-1 protease HIV-1 protease inhibitors HPLC method In-vitro In-vitro evaluation Inhibitory activity Molecular docking One pot Potent compounds Structure activity relationships Trifluoromethyl Cyclization Molecular modeling Scaffolds Synthesis (chemical) Docking Human immunodeficiency virus Human immunodeficiency virus 1 |
| Issue Date: | 2011 |
| Abstract: | Novel chromone derivatives with a benzopyran-4-one scaffold have been prepared by the one-pot cyclization reaction. The in vitro inhibitory activity of these new compounds towards HIV-1 protease have been evaluated using stop time HPLC method as the preliminary screening. The most potent compound, 7,8-dihydroxy-2-(3′-trifluoromethyl phenyl)-3-(3″- trifluoromethylbenzoyl)chromone (32), showed IC50 = 0.34 μM. The molecular docking study supported results from experimental activity testing and also provided structure-activity relationship of this series. © 2011 Elsevier B.V. All rights reserved. |
| URI: | https://ir.swu.ac.th/jspui/handle/123456789/14481 https://www.scopus.com/inward/record.uri?eid=2-s2.0-79961032360&doi=10.1016%2fj.molstruc.2011.06.035&partnerID=40&md5=007ee7698fbe2e5de50c88d3b44e8787 |
| ISSN: | 222860 |
| Appears in Collections: | Scopus 1983-2021 |
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