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.

journal_name

Bioorg Med Chem Lett

authors

Bedoya LM,del Olmo E,Sancho R,Barboza B,Beltrán M,García-Cadenas AE,Sánchez-Palomino S,López-Pérez JL,Muñoz E,San Feliciano A,Alcamí J

doi

10.1016/j.bmcl.2006.04.087

subject

Has Abstract

pub_date

2006-08-01 00:00:00

pages

4075-9

issue

15

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(06)00524-5

journal_volume

16

pub_type

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