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Molecules 2012, 17(8), 9245-9257; doi:10.3390/molecules17089245
Article

3-Phenylcoumarins as Inhibitors of HIV-1 Replication

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Received: 2 July 2012; in revised form: 25 July 2012 / Accepted: 26 July 2012 / Published: 2 August 2012
(This article belongs to the Section Medicinal Chemistry)
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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 3-phenylcoumarins; AIDS; Tat protein; NF-κB inhibition; anti-HIV activity
This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

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MDPI and ACS Style

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.

AMA Style

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.

Chicago/Turabian Style

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.



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