Title :

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

Author(s) :

Maurin, Cédric [Auteur]
Laboratoire de Chimie Organique et Macromoleculaire [UMR CNRS 8009]
Lion, Cédric [Auteur]
Laboratoire de Chimie Organique et Macromoleculaire [UMR CNRS 8009]
Bailly, Fabrice [Auteur]
Laboratoire de Chimie Organique et Macromoleculaire [UMR CNRS 8009]
Touati, Nadia [Auteur]
Laboratoire de Chimie Organique et Macromoleculaire [UMR CNRS 8009]
Vezin, Herve [Auteur]
Laboratoire de Chimie Organique et Macromoleculaire [UMR CNRS 8009]
Mbemba, Gladys [Auteur]
Laboratoire de Biotechnologie et Pharmacogénétique Appliquée [LBPA]
Mouscadet, Jean François [Auteur]
Laboratoire de Biotechnologie et Pharmacogénétique Appliquée [LBPA]
Debyser, Zeger [Auteur]
Catholic University of Leuven - Katholieke Universiteit Leuven [KU Leuven]
Witvrouw, Myriam [Auteur]
Catholic University of Leuven - Katholieke Universiteit Leuven [KU Leuven]
Cotelle, Philippe [Auteur]
Laboratoire de Chimie Organique et Macromoleculaire [UMR CNRS 8009]

Journal title :

Bioorganic & Medicinal Chemistry

Abbreviated title :

Bioorganic & Medicinal Chemistry

Volume number :

18

Pages :

5194-5201

Publisher :

Elsevier BV

Publication date :

2010-07-15

ISSN :

0968-0896

English keyword(s) :

HIV-1 Integrase inhibitors
6-Arylnaphthalene-1.2-diols

HAL domain(s) :

Chimie/Matériaux
Chimie/Chimie théorique et/ou physique

English abstract : [en]

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 ...
Show more >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.Show less >

Language :

Anglais

Peer reviewed article :

Oui

Audience :

Internationale

Popular science :

Non

Administrative institution(s) :

Université de Lille
CNRS

Collections :

• Autres travaux scientifiques

Submission date :

2021-06-18T08:40:27Z
2021-10-07T13:25:56Z
2021-10-12T16:26:09Z