Source:http://linkedlifedata.com/resource/pubmed/id/15889173
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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
10
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pubmed:dateCreated |
2005-5-12
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pubmed:abstractText |
Several water-soluble derivatives (CPT3, CPT3a-d) of camptothecin (CPT) were synthesized, among which CPT3 bearing an N,N'-dimethyl-1-aminoethylcarbamate side-chain was further conjugated with reductively eliminating structural units of indolequinone, 4-nitrobenzyl alcohol and 4-nitrofuryl alcohol to produce novel prodrugs of camptothecin (CPT4-6). All CPT derivatives were of lower cytotoxicity than their parent compound of CPT. In contrast, CPT4 and CPT6 showed higher hypoxia selectivity of cytotoxicity towards tumor cells than CPT. A mechanism by which a representative prodrug CPT4 is activated in the presence of DT-diaphorase to release CPT was also discussed. The bioreduction activated CPT prodrugs including CPT4 and CPT6 are identified to be promising for application to the hypoxia targeting tumor chemotherapy.
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pubmed:language |
eng
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pubmed:journal | |
pubmed:citationSubset |
IM
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pubmed:chemical | |
pubmed:status |
MEDLINE
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pubmed:month |
May
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pubmed:issn |
1477-0520
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pubmed:author | |
pubmed:issnType |
Print
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pubmed:day |
21
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pubmed:volume |
3
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
1905-10
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pubmed:meshHeading |
pubmed-meshheading:15889173-Antineoplastic Agents, Phytogenic,
pubmed-meshheading:15889173-Camptothecin,
pubmed-meshheading:15889173-Cell Hypoxia,
pubmed-meshheading:15889173-Cell Line, Tumor,
pubmed-meshheading:15889173-Drug Stability,
pubmed-meshheading:15889173-Humans,
pubmed-meshheading:15889173-Hydrolysis,
pubmed-meshheading:15889173-Prodrugs
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pubmed:year |
2005
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pubmed:articleTitle |
Bioreduction activated prodrugs of camptothecin: molecular design, synthesis, activation mechanism and hypoxia selective cytotoxicity.
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pubmed:affiliation |
Department of Energy and Hydrocarbon Chemistry, Graduate School of Engineering, Kyoto University, Katsura Campus, Nishikyo-ku, Kyoto, 615-8510, Japan.
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pubmed:publicationType |
Journal Article
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