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.
Keywords: 3-phenylcoumarins; AIDS; Tat protein; NF-κB inhibition; anti-HIV activity
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Olmedo, D.; Sancho, R.; Bedoya, L.M.; López-Pérez, J.L.; del Olmo, E.; Muñoz, E.; Alcamí, J.; Gupta, M.P.; San Feliciano, A. 3-Phenylcoumarins as Inhibitors of HIV-1 Replication. Molecules 2012, 17, 9245-9257.
Olmedo D, Sancho R, Bedoya LM, López-Pérez JL, del Olmo E, Muñoz E, Alcamí J, Gupta MP, San Feliciano A. 3-Phenylcoumarins as Inhibitors of HIV-1 Replication. Molecules. 2012; 17(8):9245-9257.
Olmedo, Dionisio; Sancho, Rocío; Bedoya, Luis M.; López-Pérez, José L.; del Olmo, Esther; Muñoz, Eduardo; Alcamí, José; Gupta, Mahabir P.; San Feliciano, Arturo. 2012. "3-Phenylcoumarins as Inhibitors of HIV-1 Replication." Molecules 17, no. 8: 9245-9257.