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New 2-arylnaphthalenediols and triol inhibitors of HIV-1 integrase—Discovery of a new polyhydroxylated antiviral agent
Cédric Maurin ,
Cédric Lion ,
Fabrice Bailly ,
Nadia Touati ,
Hervé Vezin ,
Gladys Mbemba ,
Jean François Mouscadet ,
Zeger Debyser ,
Myriam Witvrouw ,
Philippe Cotelle
July 2010
July 2010
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Abstract
A series of 13 hydroxylated 2-arylnaphthalenes have been synthesized and evaluated
as HIV-1 integrase inhibitors. 7-(3,4,5-trihydroxyphenyl)naphthalene-1,2,3-triol 1c
revealed chemical instability upon storage, leading to the isolation of a dimer 5c
which was also tested. In the 2-arylnaphthalene series, all compounds were active
against HIV-1 IN with IC50's within the 1-10 microM range, except for 1c and 5c which
displayed submicromolar activity. Antiviral activity against HIV-1 replication was
measured on 1b-c and 5c. Amongst the tested molecules, only 5c was found to present
antiviral properties with a low cytotoxicity on two different cell lines.