title: Antiretroviral (HIV-1) activity of azulene derivatives.
abstract: 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 8-20 μM 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.
authors.affiliation: Institute of Technology, University of Tartu, Nooruse 1, 50411 Tartu, Estonia.
authors.forename: Julia
authors.initials: J
authors.lastname: Peet
authors.affiliation: Institute of Technology, University of Tartu, Nooruse 1, 50411 Tartu, Estonia.
authors.forename: Anastasia
authors.initials: A
authors.lastname: Selyutina
authors.affiliation: Institute of Technology, University of Tartu, Nooruse 1, 50411 Tartu, Estonia. Electronic address: aleksei.bredihhin@ut.ee.
authors.forename: Aleksei
authors.initials: A
authors.lastname: Bredihhin
mesh_terms: D019380:Anti-HIV Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D052176:Azulenes / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D002460:Cell Line; D002470:Cell Survival / Q000187:drug effects; D004305:Dose-Response Relationship, Drug; D006678:HIV / Q000187:drug effects*; D006801:Humans; D008826:Microbial Sensitivity Tests; D015394:Molecular Structure; D013329:Structure-Activity Relationship; D014779:Virus Replication / Q000187:drug effects
chemical_list: D019380:Anti-HIV Agents; D052176:Azulenes; C005525:azulene
keywords: Antiviral; Azulene; HIV; HIV-1 inhibition