1240372-63-7Relevant academic research and scientific papers
New 2-arylnaphthalenediols and triol inhibitors of HIV-1 integrase - Discovery of a new polyhydroxylated antiviral agent
Maurin, Cedric,Lion, Cedric,Bailly, Fabrice,Touati, Nadia,Vezin, Herve,Mbemba, Gladys,Mouscadet, Jean Franois,Debyser, Zeger,Witvrouw, Myriam,Cotelle, Philippe
experimental part, p. 5194 - 5201 (2010/09/05)
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 μM 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.
