title: Anti-HIV activity of stilbene-related heterocyclic compounds.
abstract: Viral transcription has not been routinely targeted in the development of new antiviral drugs. This crucial step of the viral cycle depends on the concerted action of cellular and viral proteins such as NF-kappaB and Tat. In the present study, stilbene-related heterocyclic compounds including benzalphthalide, phthalazinone, imidazoindole and pyrimidoisoindole derivatives are tested for their anti-HIV activity. Original assays based on recombinant viruses were used to evaluate HIV replication inhibition and stably transfected cell lines were used to evaluate inhibition of Tat and NF-kappaB proteins. Some of the stilbene-related heterocyclic compounds analysed displayed anti-HIV activity through interference with NF-kappaB and Tat function. Moreover, compounds inhibiting both targets displayed a stronger activity on viral replication.
authors.affiliation: Unidad de Inmunopatalogía, Centro Nacional de Microbiología, Instituto de Salud Carlos III, 28220-Majadahonda, Madrid, Spain.
authors.forename: Luis M
authors.initials: LM
authors.lastname: Bedoya
authors.forename: Esther
authors.initials: E
authors.lastname: del Olmo
authors.forename: Rocío
authors.initials: R
authors.lastname: Sancho
authors.forename: Bianca
authors.initials: B
authors.lastname: Barboza
authors.forename: Manuela
authors.initials: M
authors.lastname: Beltrán
authors.forename: Ana E
authors.initials: AE
authors.lastname: García-Cadenas
authors.forename: Sonsoles
authors.initials: S
authors.lastname: Sánchez-Palomino
authors.forename: José L
authors.initials: JL
authors.lastname: López-Pérez
authors.forename: Eduardo
authors.initials: E
authors.lastname: Muñoz
authors.forename: Arturo
authors.initials: A
authors.lastname: San Feliciano
authors.forename: José
authors.initials: J
authors.lastname: Alcamí
mesh_terms: D019380:Anti-HIV Agents / Q000494:pharmacology*; D015696:Gene Products, tat / Q000037:antagonists & inhibitors; D016325:HIV Long Terminal Repeat; D006367:HeLa Cells; D006571:Heterocyclic Compounds / Q000494:pharmacology*; D006801:Humans; D016328:NF-kappa B / Q000037:antagonists & inhibitors; D013267:Stilbenes / Q000494:pharmacology*
chemical_list: D019380:Anti-HIV Agents; D015696:Gene Products, tat; D006571:Heterocyclic Compounds; D016328:NF-kappa B; D013267:Stilbenes