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

3-Phenylcoumarins as Inhibitors of HIV-1 Replication

Department of Pharmaceutical Chemistry, Faculty of Pharmacy, University of Salamanca, CIETUS-IBSAL, 37007 Salamanca, Spain
CIFLORPAN, Center for Pharmacognostic Research on Panamanian Flora, College of Pharmacy, University of Panama, Box 0824-00172, Panama, Republic of Panama
Department of Cellular Biology, Physiology and Immunology, University of Córdoba, Institute Maimonides for Biomedical Research (IMIBIC). Avda de Menendez Pidal s/n, 14004 Córdoba, Spain
National Microbiology Centre Institute Carlos III, Crt. Majadahonda a Pozuelo, 28220 Majadahonda, Madrid, Spain
Author to whom correspondence should be addressed.
Received: 2 July 2012 / Revised: 25 July 2012 / Accepted: 26 July 2012 / Published: 2 August 2012
(This article belongs to the Section Medicinal Chemistry)
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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-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. View Full-Text
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 (CC BY 3.0).

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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.

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