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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
1
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pubmed:dateCreated |
2006-3-17
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pubmed:abstractText |
Thymidine (Thd), 1-beta-D-arabinosylthymine (ara-T) and 3'-fluoro-3'-deoxythymidine (FLT) have been substituted at N-3 by a methyl or a 2-fluoroethyl group. FLT and ara-T are markedly inhibitory against human immunodeficiency virus type 1 (HIV-1) and HIV-2, and herpes simplex virus type 1 (HSV-1) and HSV-2, respectively. Modification at N-3 of these compounds markedly decreases both the antiviral and cytostatic activity of the parent compounds FLT and ara-T except for N-3-(methyl)-Thd that proved highly cytostatic for murine leukaemia L1210 cells. The decreased biological activity of the N-3-substituted pyrimidine nucleoside analogues coincides with a significantly lower affinity of the modified Thd analogues for the cellular and viral (activating) nucleoside kinases.
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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:issn |
0956-3202
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pubmed:author |
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pubmed:issnType |
Print
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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 |
17-23
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pubmed:dateRevised |
2006-11-15
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pubmed:meshHeading |
pubmed-meshheading:16542002-Animals,
pubmed-meshheading:16542002-Antineoplastic Agents,
pubmed-meshheading:16542002-Antiviral Agents,
pubmed-meshheading:16542002-Arabinonucleosides,
pubmed-meshheading:16542002-Cercopithecus aethiops,
pubmed-meshheading:16542002-Enzyme Inhibitors,
pubmed-meshheading:16542002-HeLa Cells,
pubmed-meshheading:16542002-Humans,
pubmed-meshheading:16542002-Leukemia L1210,
pubmed-meshheading:16542002-Magnetic Resonance Spectroscopy,
pubmed-meshheading:16542002-Mice,
pubmed-meshheading:16542002-Phosphotransferases,
pubmed-meshheading:16542002-Spectrometry, Mass, Electrospray Ionization,
pubmed-meshheading:16542002-Thymidine,
pubmed-meshheading:16542002-Thymine,
pubmed-meshheading:16542002-Vero Cells
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pubmed:year |
2006
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pubmed:articleTitle |
The effect of a methyl or 2-fluoroethyl substituent at the N-3 position of thymidine, 3'-fluoro-3'-deoxythymidine and 1-beta-D-arabinosylthymine on their antiviral and cytostatic activity in cell culture.
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pubmed:affiliation |
Rega Institute for Medical Research, K.U. Leuven, Leuven, Belgium. jan.balzarini@rega.kuleuven.be
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pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
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