Neoflavonoids as Inhibitors of HIV-1 Replication by Targeting the Tat and NF-κB Pathways
AbstractTwenty-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-κB and displayed anti-Tat activity simultaneously. Compounds 10, 14, and 25, inhibited HIV replication in both targets at concentrations <25 μM. 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. View Full-Text
- Supplementary File 1:
PDF-Document (PDF, 15725 KB)
Share & Cite This Article
Olmedo, D.A.; López-Pérez, J.L.; del Olmo, E.; Bedoya, L.M.; Sancho, R.; Alcamí, J.; Muñoz, E.; Feliciano, A.S.; Gupta, M.P. Neoflavonoids as Inhibitors of HIV-1 Replication by Targeting the Tat and NF-κB Pathways. Molecules 2017, 22, 321.
Olmedo DA, López-Pérez JL, del Olmo E, Bedoya LM, Sancho R, Alcamí J, Muñoz E, Feliciano AS, Gupta MP. Neoflavonoids as Inhibitors of HIV-1 Replication by Targeting the Tat and NF-κB Pathways. Molecules. 2017; 22(2):321.Chicago/Turabian Style
Olmedo, Dionisio A.; López-Pérez, José L.; del Olmo, Esther; Bedoya, Luis M.; Sancho, Rocío; Alcamí, José; Muñoz, Eduardo; Feliciano, Arturo S.; Gupta, Mahabir P. 2017. "Neoflavonoids as Inhibitors of HIV-1 Replication by Targeting the Tat and NF-κB Pathways." Molecules 22, no. 2: 321.
Note that from the first issue of 2016, MDPI journals use article numbers instead of page numbers. See further details here.