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

…, H Vezin, G Mbemba, JF Mouscadet, Z Debyser…

Index: Maurin, Cedric; Lion, Cedric; Bailly, Fabrice; Touati, Nadia; Vezin, Herve; Mbemba, Gladys; Mouscadet, Jean Franois; Debyser, Zeger; Witvrouw, Myriam; Cotelle, Philippe Bioorganic and Medicinal Chemistry, 2010 , vol. 18, # 14 p. 5194 - 5201

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Citation Number: 10

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 1–10μM range, except for 1c and 5c which displayed submicromolar ...