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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
7
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pubmed:dateCreated |
1989-11-8
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pubmed:abstractText |
The antitumor activity of 1-beta-D-arabinofuranosylcytosine-5'-alkylphosphates (CnPCAs) against L1210 leukemia in mice after oral administration was demonstrated. The optimum length of the alkyl group on the phosphate moiety of CnPCA for exhibiting a high antitumor activity was found to be between tetradecyl (C14) and tricosyl (C23). The most active alkyl derivative in this system was found to be 1-beta-D-arabinofuranosylcytosine-5'-stearylphosphate (C18PCA). The optimum and minimum effective doses of C18PCA were 100 and 6.25 mg/kg/day (q1d, day 1 to day 5), respectively. The maximum T/C% of C18PCA was approximately 220. The antitumor activity of C18PCA was not greatly dependent on the treatment schedule and route. Plasma concentration of 1-beta-D-arabinofuranosylcytosine (ara-C) remained in the range of 0.4 to 0.75 nmol/ml [corrected] for 24 h after oral administration of 100 mg/kg (170 mumol/kg) of C18PCA. These results indicate that C18PCA administered per orally is absorbed intact through the gastrointestinal tract and area-C is released of long period of time. C18PCA is regarded as an orally active depot form of ara-C.
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pubmed:commentsCorrections | |
pubmed:language |
eng
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pubmed:journal | |
pubmed:citationSubset |
IM
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pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/1-arabinofuranosylcytosine-5'-steary...,
http://linkedlifedata.com/resource/pubmed/chemical/Antineoplastic Agents,
http://linkedlifedata.com/resource/pubmed/chemical/Arabinonucleotides,
http://linkedlifedata.com/resource/pubmed/chemical/Cytarabine,
http://linkedlifedata.com/resource/pubmed/chemical/Cytidine Monophosphate,
http://linkedlifedata.com/resource/pubmed/chemical/Cytosine Nucleotides
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pubmed:status |
MEDLINE
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pubmed:month |
Jul
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pubmed:issn |
0910-5050
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pubmed:author | |
pubmed:issnType |
Print
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pubmed:volume |
80
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
679-85
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pubmed:dateRevised |
2003-11-14
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pubmed:meshHeading |
pubmed-meshheading:2507491-Administration, Oral,
pubmed-meshheading:2507491-Animals,
pubmed-meshheading:2507491-Antineoplastic Agents,
pubmed-meshheading:2507491-Arabinonucleotides,
pubmed-meshheading:2507491-Cytarabine,
pubmed-meshheading:2507491-Cytidine Monophosphate,
pubmed-meshheading:2507491-Cytosine Nucleotides,
pubmed-meshheading:2507491-Drug Administration Schedule,
pubmed-meshheading:2507491-Leukemia L1210,
pubmed-meshheading:2507491-Metabolic Clearance Rate,
pubmed-meshheading:2507491-Mice,
pubmed-meshheading:2507491-Solubility,
pubmed-meshheading:2507491-Structure-Activity Relationship
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pubmed:year |
1989
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pubmed:articleTitle |
Antitumor activity and pharmacology of 1-beta-D-arabinofuranosylcytosine-5'-stearylphosphate: an orally active derivative of 1-beta-D-arabinofuranosylcytosine.
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pubmed:affiliation |
Research Laboratories, Yamasa Shoyu Co., Ltd., Chiba.
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pubmed:publicationType |
Journal Article
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