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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
11
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pubmed:dateCreated |
2006-5-25
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pubmed:abstractText |
Molecular modeling studies and an updated highly predictive 3-D QSAR model led to the discovery of exceptionally potent indolyl aryl sulfones (IASs) characterized by the presence of either a pyrrolidyn-2-one nucleus at the indole-2-carboxamide or some substituents at the indole-2-carbohydrazide. Compounds 7 and 9 were found active in the sub-nanomolar range of concentration in both MT-4 and C8166 cell-based anti-HIV assays. These compounds, and in particular compound 9, also showed excellent inhibitory activity against both HIV-112 and HIV-AB1 primary isolates in lymphocytes and against HIV WT in macrophages.
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pubmed:language |
eng
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pubmed:journal |
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pubmed:citationSubset |
IM
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pubmed:chemical |
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pubmed:status |
MEDLINE
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pubmed:month |
Jun
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pubmed:issn |
0022-2623
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pubmed:author |
pubmed-author:ArticoMarinoM,
pubmed-author:BergaminiAlbertoA,
pubmed-author:CiapriniChiaraC,
pubmed-author:ColucciaAntonioA,
pubmed-author:CrespanEmanueleE,
pubmed-author:De MartinoGabriellaG,
pubmed-author:La ReginaGiuseppeG,
pubmed-author:LavecchiaAntonioA,
pubmed-author:MagaGiovanniG,
pubmed-author:NovellinoEttoreE,
pubmed-author:PiscitelliFrancescoF,
pubmed-author:RagnoRinoR,
pubmed-author:SilvestriRomanoR,
pubmed-author:SinistroAnnaA
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pubmed:issnType |
Print
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pubmed:day |
1
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pubmed:volume |
49
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pubmed:owner |
NLM
|
|
pubmed:authorsComplete |
Y
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pubmed:pagination |
3172-84
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pubmed:dateRevised |
2006-11-15
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pubmed:meshHeading |
pubmed-meshheading:16722636-Anti-HIV Agents,
pubmed-meshheading:16722636-Cells, Cultured,
pubmed-meshheading:16722636-Drug Design,
pubmed-meshheading:16722636-Drug Resistance, Viral,
pubmed-meshheading:16722636-HIV-1,
pubmed-meshheading:16722636-Humans,
pubmed-meshheading:16722636-Indoles,
pubmed-meshheading:16722636-Lymphocytes,
pubmed-meshheading:16722636-Macrophages,
pubmed-meshheading:16722636-Models, Molecular,
pubmed-meshheading:16722636-Pyrrolidinones,
pubmed-meshheading:16722636-Quantitative Structure-Activity Relationship,
pubmed-meshheading:16722636-Solubility,
pubmed-meshheading:16722636-Sulfones
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pubmed:year |
2006
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pubmed:articleTitle |
Design, molecular modeling, synthesis, and anti-HIV-1 activity of new indolyl aryl sulfones. Novel derivatives of the indole-2-carboxamide.
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pubmed:affiliation |
Dipartimento di Studi Farmaceutici, Istituto Pasteur-Fondazione Cenci Bolognetti, Università di Roma La Sapienza, Piazzale Aldo Moro 5, I-00185 Roma, Italy. rino.ragno@uniroma1.it
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pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
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