Anti-HIV activity of some synthetic lignanolides and intermediates

• Published in: Bioorganic & medicinal chemistry letters 2004-09, Vol.14 (17), p.4483-4486
• Main Authors: Sancho, Rocı́o, Medarde, Manuel, Sánchez-Palomino, Sonsoles, Madrigal, Blanca M, Alcamı́, José, Muñoz, Eduardo, San Feliciano, Arturo
• Format: Article
• Language: English
• Subjects: Anti-HIV Agents - chemistry; Anti-HIV Agents - metabolism; Anti-HIV Agents - pharmacology; Anti-HIV-1; Antibiotics. Antiinfectious agents. Antiparasitic agents; Antiviral agents; Biological and medical sciences; HeLa Cells; HIV-1 - drug effects; HIV-1 - physiology; HIV-1 promoter activation; HIV-1 Tat protein; Humans; Lignans - chemistry; Lignans - metabolism; Lignans - pharmacology; Medical sciences; Pharmacology. Drug treatments; Synthetic lignanolides; Transcription factor NF- κB
• ISSN: 0960-894X; 1464-3405
• DOI: 10.1016/j.bmcl.2004.06.047

The inhibitory activity of lignanolides and intermediates on HIV replication, NF- κB and Tat dependent HIV-LTR activation is evaluated. The evaluation of the anti-HIV-1 activity of synthetic lignanolides and their intermediates is reported. The antiviral activity was studied through luciferase-based assays targeting the HIV-1 promoter activation induced by either, the HIV-1 Tat protein or the cellular transcription factor NF- κB, both known as crucial factors in HIV-1 replication. Among the compounds tested, three of them 2, 4 and 13 were further analysed for their anti-HIV-1 activity by recombinant virus assays, showing a suitable profile for development of novel anti-HIV-1 drugs.