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Molecules. 2012 Aug 2;17(8):9245-57. doi: 10.3390/molecules17089245.

3-Phenylcoumarins as inhibitors of HIV-1 replication.

Author information

1
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, University of Salamanca, CIETUS-IBSAL, 37007 Salamanca, Spain.

Abstract

We have synthesized fourteen 3-phenylcoumarin derivatives and evaluated their anti-HIV activity. Antiviral activity was assessed on MT-2 cells infected with viral clones carrying the luciferase gene as reporter. Inhibition of HIV transcription and Tat function were tested on cells stably transfected with the HIV-LTR and Tat protein. Six compounds displayed NF-κB inhibition, four resulted Tat antagonists and three of them showed both activities. Three compounds inhibited HIV replication with IC₅₀ values < 25 µM. The antiviral effect of the 4-hydroxycoumarin derivative 19 correlates with its specific inhibition of Tat functions, while compound 8, 3-(2-chlorophenyl)coumarin, seems to act through a mechanism unrelated to the molecular targets considered in this research.

PMID:
22858844
PMCID:
PMC6268528
DOI:
10.3390/molecules17089245
[Indexed for MEDLINE]
Free PMC Article

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