title: Neoflavonoids as Inhibitors of HIV-1 Replication by Targeting the Tat and NF-κB Pathways.
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-one10inhibited NF-κB and displayed anti-Tat activity simultaneously. Compounds10,14, and25, 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.
authors.affiliation: Pharmaceutical Chemistry Area, Department of Pharmaceutical Sciences, University of Salamanca, Faculty of Pharmacy, CIETUS, IBSAL, Campus Miguel de Unamuno, 37007 Salamanca, Spain. dolmedoagudo@hotmail.com.
authors.forename: Dionisio A
authors.initials: DA
authors.lastname: Olmedo
authors.affiliation: Pharmaceutical Chemistry Area, Department of Pharmaceutical Sciences, University of Salamanca, Faculty of Pharmacy, CIETUS, IBSAL, Campus Miguel de Unamuno, 37007 Salamanca, Spain. lopez@usal.es.
authors.forename: José Luis
authors.initials: JL
authors.lastname: López-Pérez
authors.affiliation: Pharmaceutical Chemistry Area, Department of Pharmaceutical Sciences, University of Salamanca, Faculty of Pharmacy, CIETUS, IBSAL, Campus Miguel de Unamuno, 37007 Salamanca, Spain. olmo@usal.es.
authors.forename: Esther
authors.initials: E
authors.lastname: Del Olmo
authors.affiliation: National Centre of Microbiology, Institute Carlos III, Crt. Majadahonda a Pozuelo, 28220 Majadahonda, Madrid, Spain. lmbedoya@ucm.es.|Pharmacology Department, College of Pharmacy, Complutense University. Pz. Ramón Y Cajal s/n, 28040 Madrid, Spain. lmbedoya@ucm.es.
authors.forename: Luis M
authors.initials: LM
authors.lastname: Bedoya
authors.affiliation: Department of Cellular Biology, Physiology and Immunology, University of Córdoba, Faculty of Medicine Avda de Menendez Pidal s/n, 14004 Córdoba, Spain. Rocio.Sancho@cancer.org.uk.
authors.forename: Rocío
authors.initials: R
authors.lastname: Sancho
authors.affiliation: National Centre of Microbiology, Institute Carlos III, Crt. Majadahonda a Pozuelo, 28220 Majadahonda, Madrid, Spain. ppalcami@isciii.es.
authors.forename: José
authors.initials: J
authors.lastname: Alcamí
authors.affiliation: Department of Cellular Biology, Physiology and Immunology, University of Córdoba, Faculty of Medicine Avda de Menendez Pidal s/n, 14004 Córdoba, Spain. fi1muble@uco.es.
authors.forename: Eduardo
authors.initials: E
authors.lastname: Muñoz
authors.affiliation: Pharmaceutical Chemistry Area, Department of Pharmaceutical Sciences, University of Salamanca, Faculty of Pharmacy, CIETUS, IBSAL, Campus Miguel de Unamuno, 37007 Salamanca, Spain. artsf@usal.es.
authors.forename: Arturo San
authors.initials: AS
authors.lastname: Feliciano
authors.affiliation: CIFLORPAN, Center for Pharmacognostic Research on Panamanian Flora, College of Pharmacy, University of Panama, P.O. Box 0824-00172 Panama, Panama. mahabirpgupta@gmail.com.
authors.forename: Mahabir P
authors.initials: MP
authors.lastname: Gupta
mesh_terms: D019380:Anti-HIV Agents / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D005419:Flavonoids / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D015658:HIV Infections / Q000188:drug therapy / Q000378:metabolism / Q000821:virology; D015497:HIV-1 / Q000187:drug effects*; D006801:Humans; D008826:Microbial Sensitivity Tests; D015394:Molecular Structure; D016328:NF-kappa B / Q000378:metabolism*; D015398:Signal Transduction / Q000187:drug effects*; D014779:Virus Replication / Q000187:drug effects; D054322:tat Gene Products, Human Immunodeficiency Virus / Q000378:metabolism*
chemical_list: D019380:Anti-HIV Agents; D005419:Flavonoids; D016328:NF-kappa B; D054322:tat Gene Products, Human Immunodeficiency Virus
keywords: 4-phenyl-chromen-one; AIDS; NF-κB inhibition; Tat protein; anti-HIV activity; neoflavonoids