Abstract
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.
Highlights
UNAIDS report in 2016 indicated that tuberculosis remains the leading cause of death among people living with Human immunodeficiency virus (HIV), accounting for around one in three acquired immunodeficiency syndrome (AIDS)-related deaths
In a previous paper we reported the anti-HIV activity of natural 4-phenylcoumarins isolated from Marila pluricostata
In this paper we reported the preparation and the anti-HIV activity of several neoflavone derivatives that showed anti-mycobacterial activity [48]
Summary
UNAIDS report in 2016 indicated that tuberculosis remains the leading cause of death among people living with HIV, accounting for around one in three AIDS-related deaths. Transition from latency to HIV expression occurs mainly when cells are activated and requires the concerted action of cellular transcription factors and regulatory HIV proteins [7,8]. In a previous paper we reported the anti-HIV activity of natural 4-phenylcoumarins isolated from Marila pluricostata They were structurally related to Inophyllum coumarins series, but with one prenyl and other cyclized group across the hydroxyl group at position C-7 [43]. This relevant fact induced us to prepare new similar, but simpler, derivatives with the idea in mind to obtain compounds with activity against both. In this paper we reported the preparation and the anti-HIV activity of several neoflavone derivatives that showed anti-mycobacterial activity [48]
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