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Molecules 2017, 22(2), 321; doi:10.3390/molecules22020321

Neoflavonoids as Inhibitors of HIV-1 Replication by Targeting the Tat and NF-κB Pathways

1
Pharmaceutical Chemistry Area, Department of Pharmaceutical Sciences, University of Salamanca, Faculty of Pharmacy, CIETUS, IBSAL, Campus Miguel de Unamuno, 37007 Salamanca, Spain
2
Department of Cellular Biology, Physiology and Immunology, University of Córdoba, Faculty of Medicine Avda de Menendez Pidal s/n, 14004 Córdoba, Spain
3
CIFLORPAN, Center for Pharmacognostic Research on Panamanian Flora, College of Pharmacy, University of Panama, P.O. Box 0824-00172 Panama, Panama
4
National Centre of Microbiology, Institute Carlos III, Crt. Majadahonda a Pozuelo, 28220 Majadahonda, Madrid, Spain
5
Pharmacology Department, College of Pharmacy, Complutense University. Pz. Ramón Y Cajal s/n, 28040 Madrid, Spain
*
Authors to whom correspondence should be addressed.
Academic Editor: Derek J. McPhee
Received: 12 January 2017 / Revised: 19 January 2017 / Accepted: 16 February 2017 / Published: 19 February 2017
(This article belongs to the Section Bioorganic Chemistry)
View Full-Text   |   Download PDF [794 KB, uploaded 23 February 2017]   |  

Abstract

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-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
Keywords: neoflavonoids; 4-phenyl-chromen-one; AIDS; Tat protein; NF-κB inhibition; anti-HIV activity neoflavonoids; 4-phenyl-chromen-one; AIDS; Tat protein; NF-κB inhibition; anti-HIV activity
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

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MDPI and ACS Style

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.

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