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Neoflavonoids as Inhibitors of HIV-1 Replication by Targeting the Tat and NF-κB Pathways Olmedo, Dionisio A. López-Pérez, José Luis del Olmo, Esther Bedoya Del Olmo, Luis Miguel Sancho, Rocío Alcamí, José Muñoz, Eduardo San Feliciano, Arturo Gupta, Mahabir P. 615.011 Neoflavonoids 4-phenyl-chromen-one AIDS Tat protein NF-κB inhibition Anti-HIV activity Farmacología (Farmacia) Química farmaceútica 3209 Farmacología 2390 Química Farmacéutica Twenty-eight neoflavonoids have been prepared and evaluated in vitro against HIV-1. Antiviral activity was assessed on MT-2 cells infected with viral clones carrying the luciferase reporter gene. Inhibition of HIV transcription and Tat function were tested on cells stably transfected with the HIV-LTR and Tat protein. Seven 4-phenylchromen-2 one derivatives showed HIV transcriptional inhibitory activity but only the phenylchrome-2-one 10 inhibited NF-κB and displayed anti-Tat activity simultaneously. Compounds 10, 14, and 25, inhibited HIV replication in both targets at concentrations <25 µM. The assays of these synthetic 4 phenylchromen-2-ones may aid in the investigation of some aspects of the anti-HIV activity of such compounds and could serve as a scaffold for designing better anti-HIV compounds, which may lead to a potential anti-HIV therapeutic drug. Ministerio de Economía, Comercio y Empresa (España)/Instituto de Salud Carlos III/Fondo Europeo de Desarrollo Regional Instituto de Salud Carlos III/Fondo Europeo de Desarrollo Regional Depto. de Farmacología, Farmacognosia y Botánica Fac. de Farmacia TRUE pub 2023-06-18T00:05:44Z 2023-06-18T00:05:44Z 2017-02-19 journal article https://hdl.handle.net/20.500.14352/19242 1420-3049 10.3390/molecules22020321 eng PI16/CIII/034 RD16CIII/0002/0001 Olmedo, D. A., López-Pérez, J. L., Del Olmo, E. et al. «Neoflavonoids as Inhibitors of HIV-1 Replication by Targeting the Tat and NF-κB Pathways». Molecules, vol. 22, n.o 2, febrero de 2017, p. 321. DOI.org (Crossref), https://doi.org/10.3390/molecules22020321. Atribución 3.0 España https://creativecommons.org/licenses/by/3.0/es/ open access application/pdf MDPI