Source:http://linkedlifedata.com/resource/pubmed/id/15027876
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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
7
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pubmed:dateCreated |
2004-3-18
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pubmed:abstractText |
A group of 3'-O- and 5'-O-(3-benzenesulfonylfuroxan-4-yl)-2'-deoxyuridines possessing a variety of substituents (H, Me, I, F, CF(3)) at the C-5 position of the nucleoside moiety were synthesized for evaluation as hybrid anticancer agents that have the ability to simultaneously release cytotoxic nitric oxide (*NO). Incubation of these nitric oxide donor-nucleoside conjugates in the presence of 18 mM L-cysteine released a high percentage of *NO (21-48% at 1 h; 37-86% at 16 h). The release of *NO in the absence of the thiol cofactor was negligible. These hybrid *NO donor-nucleosides exhibited high cellular toxicity (CC(50) = 10(-6)-10(-8) M range) against a battery of tumor cell lines (143B-LTK, 143B, EMT-6, KBALB-STK, and KBALB) and normal human fibroblasts (Hs578Bst). No differences in cytotoxicity between nontransfected (143B, KBALB) and the corresponding transfected (143B-LTK, KBALB-STK) cancer cell lines possessing the herpes simplex virus type 1 (HSV-1) thymidine kinase gene (TK(+)) were observed, indicating that expression of the viral TK enzyme did not provide a gene therapeutic effect.
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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/Antineoplastic Agents,
http://linkedlifedata.com/resource/pubmed/chemical/Nitric Oxide Donors,
http://linkedlifedata.com/resource/pubmed/chemical/Oxadiazoles,
http://linkedlifedata.com/resource/pubmed/chemical/Uridine,
http://linkedlifedata.com/resource/pubmed/chemical/furoxans
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pubmed:status |
MEDLINE
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pubmed:month |
Mar
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pubmed:issn |
0022-2623
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pubmed:author | |
pubmed:issnType |
Print
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pubmed:day |
25
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pubmed:volume |
47
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
1840-6
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pubmed:dateRevised |
2006-11-15
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pubmed:meshHeading |
pubmed-meshheading:15027876-Animals,
pubmed-meshheading:15027876-Antineoplastic Agents,
pubmed-meshheading:15027876-Cell Line,
pubmed-meshheading:15027876-Cell Line, Tumor,
pubmed-meshheading:15027876-Drug Screening Assays, Antitumor,
pubmed-meshheading:15027876-Humans,
pubmed-meshheading:15027876-Mice,
pubmed-meshheading:15027876-Nitric Oxide Donors,
pubmed-meshheading:15027876-Oxadiazoles,
pubmed-meshheading:15027876-Structure-Activity Relationship,
pubmed-meshheading:15027876-Uridine
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pubmed:year |
2004
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pubmed:articleTitle |
Design and synthesis of 3'- and 5'-O-(3-benzenesulfonylfuroxan-4-yl)-2'-deoxyuridines: biological evaluation as hybrid nitric oxide donor-nucleoside anticancer agents.
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pubmed:affiliation |
Faculty of Pharmacy and Pharmaceutical Sciences, University of Alberta, Edmonton, Alberta, T6G 2N8 Canada.
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pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
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