Source:http://linkedlifedata.com/resource/pubmed/id/20541944
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
14
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pubmed:dateCreated |
2010-7-13
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pubmed:abstractText |
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.
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pubmed:language |
eng
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pubmed:journal | |
pubmed:citationSubset |
IM
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pubmed:chemical | |
pubmed:status |
MEDLINE
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pubmed:month |
Jul
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pubmed:issn |
1464-3391
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pubmed:author |
pubmed-author:BaillyFabriceF,
pubmed-author:CotellePhilippeP,
pubmed-author:DebyserZegerZ,
pubmed-author:LionCédricC,
pubmed-author:MaurinCédricC,
pubmed-author:MbembaGladysG,
pubmed-author:MouscadetJean FrançoisJF,
pubmed-author:TouatiNadiaN,
pubmed-author:VezinHervéH,
pubmed-author:WitvrouwMyriamM
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pubmed:copyrightInfo |
Copyright (c) 2010 Elsevier Ltd. All rights reserved.
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pubmed:issnType |
Electronic
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pubmed:day |
15
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pubmed:volume |
18
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
5194-201
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pubmed:meshHeading |
pubmed-meshheading:20541944-Anti-HIV Agents,
pubmed-meshheading:20541944-Cell Line,
pubmed-meshheading:20541944-Cell Survival,
pubmed-meshheading:20541944-HIV Infections,
pubmed-meshheading:20541944-HIV Integrase Inhibitors,
pubmed-meshheading:20541944-HIV-1,
pubmed-meshheading:20541944-Humans,
pubmed-meshheading:20541944-Naphthalenes
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pubmed:year |
2010
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pubmed:articleTitle |
New 2-arylnaphthalenediols and triol inhibitors of HIV-1 integrase--discovery of a new polyhydroxylated antiviral agent.
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pubmed:affiliation |
Laboratoire de Chimie Organique et Macromoléculaire, UMR CNRS 8009, Université des Sciences et Technologies de Lille, 59655 Villeneuve d'Ascq, France.
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pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
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