Neoflavonoids as Inhibitors of HIV-1 Replication by Targeting the Tat and NF-κB Pathways.
Molecules
; 22(2)2017 Feb 19.
Article
em En
| MEDLINE
| ID: mdl-28218730
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.
Palavras-chave
Texto completo:
1
Base de dados:
MEDLINE
Assunto principal:
Flavonoides
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Transdução de Sinais
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NF-kappa B
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HIV-1
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Fármacos Anti-HIV
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Produtos do Gene tat do Vírus da Imunodeficiência Humana
Limite:
Humans
Idioma:
En
Ano de publicação:
2017
Tipo de documento:
Article