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Bioorg Med Chem Lett. 2005 Oct 15;15(20):4447-50.

4-Phenylcoumarins as HIV transcription inhibitors.

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Unidad de Inmunopatalogía, Centro Nacional de Microbiología, Instituto de Salud Carlos III, 28220-Majadahonda, Madrid, Spain.


We have evaluated the anti-HIV activity of eleven natural 4-phenylcoumarins isolated from Marila pluricostata and three of their derivatives. Antiviral activity was assessed on MT-2 cells infected with viral clones carrying the luciferase gene as reporter. Inhibitions of HIV transcription and Tat function were tested on cells stably transfected with the HIV-LTR and Tat protein. Most of the coumarins tested displayed NF-kappaB inhibition. Two coumarins were also Tat antagonists and the presence of both activities correlated with a stronger inhibition of HIV replication. Our results show that antiviral effect of 4-phenylcoumarins can be related to the inhibition of NF-kappaB and Tat, and suggest that these types of compounds can be useful in the treatment of HIV infection as viral transcription inhibitors.

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