Journal
MOLECULES
Volume 17, Issue 8, Pages 9245-9257Publisher
MDPI
DOI: 10.3390/molecules17089245
Keywords
3-phenylcoumarins; AIDS; Tat protein; NF-kappa B inhibition; anti-HIV activity
Funding
- Spanish Health Ministry [RETICS RD06/0006, RD06/0021/0022]
- Instituto de Salud Carlos III [PI05/1526, PI06/0782, PI08/0752]
- FIPSE [36630/07]
- VIRHOST Network from Comunidad de Madrid
- National Secretariat of Science, Technolgy and Innovation (SENACYT)
- University of Panama under the Programa Iberoamericano CYTED. Subprograma X
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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-kappa B inhibition, four resulted Tat antagonists and three of them showed both activities. Three compounds inhibited HIV replication with IC50 values < 25 mu M. 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.
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