2. Academic Validation
  3. New 2-arylnaphthalenediols and triol inhibitors of HIV-1 integrase--discovery of a new polyhydroxylated antiviral agent

New 2-arylnaphthalenediols and triol inhibitors of HIV-1 integrase--discovery of a new polyhydroxylated antiviral agent

  • Bioorg Med Chem. 2010 Jul 15;18(14):5194-201. doi: 10.1016/j.bmc.2010.05.059.
Cédric Maurin 1,  Cédric Lion,  Fabrice Bailly,  Nadia Touati,  Hervé Vezin,  Gladys Mbemba,  Jean François Mouscadet,  Zeger Debyser,  Myriam Witvrouw,  Philippe Cotelle
Affiliations

Affiliation

  • 1 Laboratoire de Chimie Organique et Macromoléculaire, UMR CNRS 8009, Université des Sciences et Technologies de Lille, 59655 Villeneuve d'Ascq, France.
PMID: 20541944 DOI: 10.1016/j.bmc.2010.05.059
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.

Figures