Neoflavonoids as Inhibitors of HIV-1 Replication by Targeting the Tat and NF-κB Pathways



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Olmedo, Dionisio A. and López-Pérez, José Luis and del Olmo, Esther and Bedoya del Olmo, Luis Miguel and Sancho, Rocío and Alcamí, José and Muñoz, Eduardo and San Feliciano, Arturo and Gupta, Mahabir P. (2017) Neoflavonoids as Inhibitors of HIV-1 Replication by Targeting the Tat and NF-κB Pathways. Molecules, 22 (2). p. 321. ISSN 1420-3049

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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.

Item Type:Article
Uncontrolled Keywords:neoflavonoids; 4-phenyl-chromen-one; AIDS; Tat protein; NF-κB inhibition; anti-HIV activity
Subjects:Medical sciences > Pharmacy > Pharmacology
Medical sciences > Pharmacy > Pharmaceutical chemistry
ID Code:69186
Deposited On:15 Dec 2021 13:37
Last Modified:20 Dec 2021 08:50

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