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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
3
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pubmed:dateCreated |
1997-10-23
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pubmed:abstractText |
We investigated structure-activity relationships of 5-substituted uracil nucleoside analogues for their selective antiviral activity against varicella-zoster virus (VZV) and affinity for VZV thymidine kinase (TK). Anti-proliferative activity of the compounds was measured using human lymphoblastoid cells. Most 2'-deoxyribofuranosyluracil, arabinofuranosyluracil (araU) and 2'-deoxy-2'-fluoro-arabinofuranosyluracil derivatives showed selective anti-VZV activity as well as activity against herpes simplex virus types 1 and 2. 2'-Deoxyuridine derivatives showed higher affinity than the corresponding araU analogues. A correlation was seen between the 50% effective doses for VZV and the Ki values for VZV TK, except for 5-ethyl-2'-deoxyuridine and 5-ethyl araU that showed relatively high affinity for VZV TK without showing any activity against VZV. 5-Halogenovinyluracil nucleosides showed the highest affinity and the most potent and selective anti-VZV activity. 2'-Deoxy-2'-fluoro-arabinofuranosyluracil derivatives exhibited high anti-VZV potency though they showed relatively low affinity for VZV TK. Some 3'-deoxythymidine analogues having anti-human immunodeficiency virus activity were inactive against herpesviruses.
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pubmed:language |
eng
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pubmed:journal | |
pubmed:citationSubset |
IM
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pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/5-bromo-6-ethoxy-5,6-dihydro-2',3'-i...,
http://linkedlifedata.com/resource/pubmed/chemical/Antineoplastic Agents,
http://linkedlifedata.com/resource/pubmed/chemical/Antiviral Agents,
http://linkedlifedata.com/resource/pubmed/chemical/Arabinofuranosyluracil,
http://linkedlifedata.com/resource/pubmed/chemical/Arabinonucleosides,
http://linkedlifedata.com/resource/pubmed/chemical/Deoxyuracil Nucleotides,
http://linkedlifedata.com/resource/pubmed/chemical/Growth Inhibitors,
http://linkedlifedata.com/resource/pubmed/chemical/Thymidine Kinase,
http://linkedlifedata.com/resource/pubmed/chemical/Uridine
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pubmed:status |
MEDLINE
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pubmed:month |
Aug
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pubmed:issn |
0166-3542
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pubmed:author | |
pubmed:issnType |
Print
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pubmed:volume |
35
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
167-75
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pubmed:dateRevised |
2007-11-15
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pubmed:meshHeading |
pubmed-meshheading:9298756-Antineoplastic Agents,
pubmed-meshheading:9298756-Antiviral Agents,
pubmed-meshheading:9298756-Arabinofuranosyluracil,
pubmed-meshheading:9298756-Arabinonucleosides,
pubmed-meshheading:9298756-Deoxyuracil Nucleotides,
pubmed-meshheading:9298756-Growth Inhibitors,
pubmed-meshheading:9298756-Herpesvirus 3, Human,
pubmed-meshheading:9298756-Humans,
pubmed-meshheading:9298756-Precursor Cell Lymphoblastic Leukemia-Lymphoma,
pubmed-meshheading:9298756-Structure-Activity Relationship,
pubmed-meshheading:9298756-Thymidine Kinase,
pubmed-meshheading:9298756-Tumor Cells, Cultured,
pubmed-meshheading:9298756-Uridine
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pubmed:year |
1997
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pubmed:articleTitle |
Structure-activity relationship of the affinity of 5-substituted uracil nucleoside analogues for varicella-zoster virus thymidine kinase and their activity against varicella-zoster virus.
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pubmed:affiliation |
Biochemicals Division, Yamasa Corporation, Choshi, Japan.
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pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
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