3-Phenylcoumarins as Inhibitors of HIV-1 Replication
Bedoya, Luis M.
López-Pérez, José L.
Olmo, Esther del
Gupta, Mahabir P.
San Feliciano, Arturo
METS:Mostrar el registro METS
PREMIS:Mostrar el registro PREMIS
MetadatosMostrar el registro completo del ítem
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.