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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
8
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pubmed:dateCreated |
1983-9-9
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pubmed:abstractText |
A glyceride derivative of chlorambucil (2), 1,3-dipalmitoyl-2-[4-[bis (2-chloroethyl)amino]benzenebutanoyl]glycerol (1), was synthesized and tested as an orally administrable antineoplastic drug endowed with lymphotropic properties. A significantly higher efficacy (increased life span) and a reduced toxicity of 1, relative to 2, were apparent when both compounds given per os were evaluated against P388 leukemia subcutaneously implanted in mice, a situation where the tumor cells disseminate along the lymphatic route. In order to assess the selective absorption of 1 by the intestinal lymphatic system after oral administration, we determined plasma and intestinal lymphatic concentrations and compared them with that obtained with 2. The results clearly demonstrate that the esterification of 2 to a diacylglycerol moiety brings about considerably higher levels in the lymph and reduces plasma levels. Moreover, pharmacokinetic and biological data suggest that 1 is most probably acting by itself rather than as a prodrug of chlorambucil.
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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 |
Aug
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pubmed:issn |
0022-2623
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pubmed:author | |
pubmed:issnType |
Print
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pubmed:volume |
26
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
1200-3
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pubmed:dateRevised |
2006-11-15
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pubmed:meshHeading |
pubmed-meshheading:6876088-Administration, Oral,
pubmed-meshheading:6876088-Animals,
pubmed-meshheading:6876088-Antineoplastic Agents,
pubmed-meshheading:6876088-Cell Survival,
pubmed-meshheading:6876088-Chlorambucil,
pubmed-meshheading:6876088-Intestines,
pubmed-meshheading:6876088-Leukemia P388,
pubmed-meshheading:6876088-Lymph Nodes,
pubmed-meshheading:6876088-Male,
pubmed-meshheading:6876088-Mice,
pubmed-meshheading:6876088-Rats,
pubmed-meshheading:6876088-Rats, Inbred Strains
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pubmed:year |
1983
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pubmed:articleTitle |
1,3-dipalmitoylglycerol ester of chlorambucil as a lymphotropic, orally administrable antineoplastic agent.
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pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
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