Quinoline-based compounds as modulators of HIV transcription through NF-κB and Sp1 inhibition

18 quinoline-based compounds were tested for antiviral properties against human immunodeficiency syndrome (HIV). The compounds tested here contain quinoline or tetrahydroquinoline rings and can be divided into two main groups: group 1 includes 4-(2-oxopyrrolidinyl-1)-1,2,3,4-tetrahydroquinolines wit...

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Bibliographic Details
Published in:Antiviral research 2010-09, Vol.87 (3), p.338-344
Main Authors: Bedoya, Luis Miguel, Abad, María José, Calonge, Esther, Saavedra, Luis Astudillo, Gutierrez C., Margarita, Kouznetsov, Vladimir V., Alcami, José, Bermejo, Paulina
Format: Article
Language:English
Subjects:
12-O-Tetradecanoylphorbol-13-acetate
AIDS
Antibiotics. Antiinfectious agents. Antiparasitic agents
Antiviral
Antiviral agents
Biological and medical sciences
HIV
Human immunodeficiency virus
Human viral diseases
Immunodeficiencies
Immunodeficiencies. Immunoglobulinopathies
Immunopathology
Infectious diseases
Medical sciences
Pharmacology. Drug treatments
Quinoline derivatives
Viral diseases
Viral diseases of the lymphoid tissue and the blood. Aids
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Summary:18 quinoline-based compounds were tested for antiviral properties against human immunodeficiency syndrome (HIV). The compounds tested here contain quinoline or tetrahydroquinoline rings and can be divided into two main groups: group 1 includes 4-(2-oxopyrrolidinyl-1)-1,2,3,4-tetrahydroquinolines with 2-(3-nitrophenyl) substituent (N-series) or 2-(3-aminophenyl) moiety (H-series), and group 2 includes 2-(3-nitrophenyl)- or 2-(3-aminophenyl)-substituted quinolines (S-series). Two different antiviral assays were performed in order to test the anti-HIV activity of compounds: 3-(4,5-dimethyl-thiazol-2-yl)-2,5-diphenyl tetrazolium bromide (MTT) and recombinant virus assay (RVA). Results showed that the most active compounds were 2-aryl quinolines, particularly those containing methoxy substituents or no substituents in the quinoline skeleton. HIV transcription inhibition appears to be their target in both resting and phorbol myristate acetate (PMA) activated primary lymphocytes, and nuclear factor-κB (NF-κB) and specificity protein-1 (SP1) seems to be the most important transcription factors involved in their action.
ISSN:0166-3542
1872-9096
DOI:10.1016/j.antiviral.2010.06.006