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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
9
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pubmed:dateCreated |
2007-4-6
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pubmed:abstractText |
The synthesis of bifunctional compound 10 consisting of d4U joined at C-5 to a butynyl spacer attached to HI-236 is reported using a Sonogashira coupling as a key step. As a non-cleavable bifunctional HIV inhibitor incorporating an NRTI with an NNRTI, 10 shows good inhibitory activity (EC(50)=250 nM) against HIV (IIIB) replication in MT-2 cell culture, which is eight times greater than that of d4T and between those of the two component drugs.
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pubmed:grant |
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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 |
May
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pubmed:issn |
0960-894X
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pubmed:author |
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pubmed:issnType |
Print
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pubmed:day |
1
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pubmed:volume |
17
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
2614-7
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pubmed:dateRevised |
2007-11-15
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pubmed:meshHeading |
pubmed-meshheading:17317163-Anti-HIV Agents,
pubmed-meshheading:17317163-Cell Line,
pubmed-meshheading:17317163-Chemistry, Pharmaceutical,
pubmed-meshheading:17317163-Dimerization,
pubmed-meshheading:17317163-Drug Design,
pubmed-meshheading:17317163-HIV Reverse Transcriptase,
pubmed-meshheading:17317163-Humans,
pubmed-meshheading:17317163-Models, Chemical,
pubmed-meshheading:17317163-Molecular Conformation,
pubmed-meshheading:17317163-Nucleosides,
pubmed-meshheading:17317163-Pyridines,
pubmed-meshheading:17317163-Reverse Transcriptase Inhibitors,
pubmed-meshheading:17317163-Thiourea,
pubmed-meshheading:17317163-Virus Replication
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pubmed:year |
2007
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pubmed:articleTitle |
[d4U]-butyne-[HI-236] as a non-cleavable, bifunctional NRTI/NNRTI HIV-1 reverse-transcriptase inhibitor.
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pubmed:affiliation |
Department of Chemistry, University of Cape Town, Rondebosch 7701, South Africa. Roger.Hunter@uct.ac.za
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pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't,
Research Support, N.I.H., Extramural
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