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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
12
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pubmed:dateCreated |
1981-3-24
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pubmed:abstractText |
A number of N-acyl and N-(alkoxycarbonyl)-5-fluorouracil derivatives possessing, for example, benzoyl, o-toluyl, acetyl, propionyl, heptanoyl, ethoxycarbonyl, phenoxycarbonyl, and benzyloxycarbonyl groups as N1 and/or N3 substituents were synthesized, and their antitumor activities were evaluated. The synthesis was achieved by a direct and two-step acylation of 5-fluorouracil and by selective N1-deacetylation of N1-acetyl-N3-substituted-5-fluorouracil under appropriate reaction conditions. Several N3-benzoyl- and N3-o-toluyl-5-fluorouracil derivates and showed significant activity against experimental tumor, and N1-acetyl-N3-o-toluyl-5-fluorouracil was found to be most promising among them. Further investigation revealed 12 to retain higher activity toward various tumors, with lower toxicity and good blood level, than either 1 or FT-207, even for oral administration.
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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 |
Dec
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pubmed:issn |
0022-2623
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pubmed:author |
pubmed-author:FukawaKK,
pubmed-author:HagaSS,
pubmed-author:HiiragiMM,
pubmed-author:IrinoOO,
pubmed-author:KametaniTT,
pubmed-author:KigasawaKK,
pubmed-author:NagamatsuYY,
pubmed-author:NakayamaMM,
pubmed-author:NishimuraNN,
pubmed-author:OkadaTT,
pubmed-author:SugiHH,
pubmed-author:TaguchiAA,
pubmed-author:WakisakaKK,
pubmed-author:YamamotoTT
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pubmed:issnType |
Print
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pubmed:volume |
23
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pubmed:owner |
NLM
|
pubmed:authorsComplete |
Y
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pubmed:pagination |
1324-9
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pubmed:dateRevised |
2008-11-21
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pubmed:meshHeading |
pubmed-meshheading:7452684-Animals,
pubmed-meshheading:7452684-Antineoplastic Agents,
pubmed-meshheading:7452684-Chemical Phenomena,
pubmed-meshheading:7452684-Chemistry,
pubmed-meshheading:7452684-Female,
pubmed-meshheading:7452684-Fluorouracil,
pubmed-meshheading:7452684-Lethal Dose 50,
pubmed-meshheading:7452684-Leukemia P388,
pubmed-meshheading:7452684-Mice,
pubmed-meshheading:7452684-Neoplasms, Experimental
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pubmed:year |
1980
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pubmed:articleTitle |
Studies on the synthesis of chemotherapeutics. 10. Synthesis and antitumor activity of N-acyl- and N-(alkoxycarbonyl)-5-fluorouracil derivatives.
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pubmed:publicationType |
Journal Article
|