Neoflavonoids as Inhibitors of HIV-1 Replication by Targeting the Tat and NF-kB Pathways
Autor
Olmedo, Dionisio
López-Pérez, José L.
Olmo, Esther del
Bedoya, Luis M.
Sancho, Rocío
Alcamí, José
Muñoz, Eduardo
San Feliciano, Arturo
Gupta, Mahabir P.
Editor
MDPIFecha
2017Materia
Neoflavonoids4-phenyl-chromen-one
AIDS
Tat protein
NF-kB inhibition
Anti-HIV activity
METS:
Mostrar el registro METSPREMIS:
Mostrar el registro PREMISMetadatos
Mostrar el registro completo del ítemResumen
Twenty-eight neoflavonoids have been prepared and evaluated in vitro against HIV-1.
Antiviral activity was assessed on MT-2 cells infected with viral clones carrying the luciferase reporter
gene. Inhibition of HIV transcription and Tat function were tested on cells stably transfected with the
HIV-LTR and Tat protein. Seven 4-phenylchromen-2-one derivatives showed HIV transcriptional
inhibitory activity but only the phenylchrome-2-one 10 inhibited NF- B and displayed anti-Tat activity
simultaneously. Compounds 10, 14, and 25, inhibited HIV replication in both targets at concentrations
<25 M. The assays of these synthetic 4-phenylchromen-2-ones may aid in the investigation of some
aspects of the anti-HIV activity of such compounds and could serve as a scaffold for designing better
anti-HIV compounds, which may lead to a potential anti-HIV therapeutic drug