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rdf:type |
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lifeskim:mentions |
umls-concept:C0003451,
umls-concept:C0018544,
umls-concept:C0019704,
umls-concept:C0021236,
umls-concept:C0035820,
umls-concept:C0038761,
umls-concept:C0184511,
umls-concept:C0243071,
umls-concept:C0441655,
umls-concept:C0567415,
umls-concept:C1260969,
umls-concept:C1373120
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|
pubmed:issue |
20
|
|
pubmed:dateCreated |
2007-9-27
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|
pubmed:abstractText |
Indolyl aryl sulfones bearing the 4,5-difluoro (10) or 5-chloro-4-fluoro (16) substitution pattern at the indole ring were potent inhibitors of HIV-1 WT and the NNRTI-resistant strains Y181C and K103N-Y181C. These compounds were highly effective against the 112 and the AB1 strains in lymphocytes and inhibited at nanomolar concentration the multiplication of the IIIBBa-L strain in macrophages. Compound 16 was exceptionally potent against RT WT and RTs carrying the K103N, Y181I, and L100I mutations.
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pubmed:language |
eng
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pubmed:journal |
|
|
pubmed:citationSubset |
IM
|
|
pubmed:chemical |
|
|
pubmed:status |
MEDLINE
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pubmed:month |
Oct
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pubmed:issn |
0022-2623
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pubmed:author |
pubmed-author:ArticoMarinoM,
pubmed-author:BergaminiAlbertoA,
pubmed-author:CavazzaAntonellaA,
pubmed-author:ColucciaAntonioA,
pubmed-author:MagaGiovanniG,
pubmed-author:NovellinoEttoreE,
pubmed-author:PiscitelliFrancescoF,
pubmed-author:ReginaGiuseppe LaGL,
pubmed-author:SamueleAlbertaA,
pubmed-author:SilvestriRomanoR,
pubmed-author:SinistroAnnaA,
pubmed-author:ZanoliSamanthaS
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|
pubmed:issnType |
Print
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pubmed:day |
4
|
|
pubmed:volume |
50
|
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pubmed:owner |
NLM
|
|
pubmed:authorsComplete |
Y
|
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pubmed:pagination |
5034-8
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pubmed:meshHeading |
pubmed-meshheading:17803291-Cell Line,
pubmed-meshheading:17803291-Drug Resistance, Viral,
pubmed-meshheading:17803291-HIV Reverse Transcriptase,
pubmed-meshheading:17803291-HIV-1,
pubmed-meshheading:17803291-Humans,
pubmed-meshheading:17803291-Indoles,
pubmed-meshheading:17803291-Lymphocytes,
pubmed-meshheading:17803291-Macrophages,
pubmed-meshheading:17803291-Reverse Transcriptase Inhibitors,
pubmed-meshheading:17803291-Structure-Activity Relationship,
pubmed-meshheading:17803291-Sulfones
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pubmed:year |
2007
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pubmed:articleTitle |
Indolyl aryl sulfones as HIV-1 non-nucleoside reverse transcriptase inhibitors: role of two halogen atoms at the indole ring in developing new analogues with improved antiviral activity.
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|
pubmed:affiliation |
Istituto Pasteur--Fondazione Cenci Bolognetti, Dipartimento di Studi Farmaceutici, Sapienza Università di Roma, Piazzale Aldo Moro 5, I-00185 Roma, Italy.
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pubmed:publicationType |
Journal Article,
In Vitro,
Research Support, Non-U.S. Gov't
|
