Antiretroviral (HIV-1) activity of azulene derivatives

[Display omitted] The antiretroviral activity of azulene derivatives was detected for the first time. A series of eighteen diversely substituted azulenes was synthesized and tested in vitro using HIV-1 based virus-like particles (VLPs) and infectious HIV-1 virus in U2OS and TZM-bl cell lines. Among...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry 2016-04, Vol.24 (8), p.1653-1657
Main Authors: Peet, Julia, Selyutina, Anastasia, Bredihhin, Aleksei
Format: Article
Language:English
Subjects:
Anti-HIV Agents - chemical synthesis
Anti-HIV Agents - chemistry
Anti-HIV Agents - pharmacology
Antiviral
Azulene
Azulenes - chemical synthesis
Azulenes - chemistry
Azulenes - pharmacology
Cell Line
Cell Survival - drug effects
Dose-Response Relationship, Drug
HIV
HIV - drug effects
HIV-1 inhibition
Human immunodeficiency virus 1
Humans
Microbial Sensitivity Tests
Molecular Structure
Structure-Activity Relationship
Virus Replication - drug effects
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Summary:[Display omitted] The antiretroviral activity of azulene derivatives was detected for the first time. A series of eighteen diversely substituted azulenes was synthesized and tested in vitro using HIV-1 based virus-like particles (VLPs) and infectious HIV-1 virus in U2OS and TZM-bl cell lines. Among the compounds tested, the 2-hydroxyazulenes demonstrated the most significant activity by inhibiting HIV-1 replication with IC50 of 2–10 and 8–20μM for the VLPs and the infectious virus, respectively. These results indicate that azulene derivatives may be potentially useful candidates for the development of antiretroviral agents.
ISSN:0968-0896
1464-3391
DOI:10.1016/j.bmc.2016.02.038