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3-Phenylcoumarins as Inhibitors of HIV-1 Replication
dc.contributor.author | Olmedo, Dionisio | |
dc.contributor.author | Sancho, Rocío | |
dc.contributor.author | Bedoya, Luis M. | |
dc.contributor.author | López-Pérez, José L. | |
dc.contributor.author | Olmo, Esther del | |
dc.contributor.author | Muñoz, Eduardo | |
dc.contributor.author | Gupta, Mahabir P. | |
dc.contributor.author | San Feliciano, Arturo | |
dc.contributor.author | Alcamí, José | |
dc.date.accessioned | 2017-11-06T13:08:32Z | |
dc.date.available | 2017-11-06T13:08:32Z | |
dc.date.issued | 2012 | |
dc.identifier.uri | http://hdl.handle.net/10396/15313 | |
dc.description.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. | es_ES |
dc.format.mimetype | application/pdf | es_ES |
dc.language.iso | eng | es_ES |
dc.publisher | MDPI | es_ES |
dc.rights | https://creativecommons.org/licenses/by/4.0/ | es_ES |
dc.source | Molecules 17(8), 9245-9257 (2012) | es_ES |
dc.subject | 3-phenylcoumarins | es_ES |
dc.subject | AIDS | es_ES |
dc.subject | Tat protein | es_ES |
dc.subject | NF-κB inhibition | es_ES |
dc.subject | Anti-HIV activity | es_ES |
dc.title | 3-Phenylcoumarins as Inhibitors of HIV-1 Replication | es_ES |
dc.type | info:eu-repo/semantics/article | es_ES |
dc.relation.publisherversion | http://dx.doi.org/10.3390/molecules17089245 | es_ES |
dc.relation.projectID | Gobierno de España. RD06/0006 (RETICS) | es_ES |
dc.relation.projectID | Gobierno de España. RD06/0021/0022 (RETICS) | es_ES |
dc.relation.projectID | Instituto de Salud Carlos III. PI05/1526 | es_ES |
dc.relation.projectID | Instituto de Salud Carlos III. PI06/0782 | es_ES |
dc.relation.projectID | Instituto de Salud Carlos III. PI08/0752 | es_ES |
dc.rights.accessRights | info:eu-repo/semantics/openAccess | es_ES |