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

作者：Maurin Cedric; Lion Cedric; Bailly Fabrice; Touati Nadia; Vezin Herve; Mbemba Gladys; Mouscadet Jean Francois; Debyser Zeger; Witvrouw Myriam; Cotelle Philippe^*

来源：Bioorganic & Medicinal Chemistry, 2010, 18(14): 5194-5201.

DOI：10.1016/j.bmc.2010.05.059

• 6-Arylnaphthalene-1,2-diols
• HIV-1 Integrase inhibitors

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 lM 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.

• 出版日期2010-7-15