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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
4
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pubmed:dateCreated |
2002-3-7
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pubmed:abstractText |
Two 4'-propylcarbonoxy derivatives (2,3) of etoposide (1), a topoisomerase II inhibitor, were synthesized and evaluated as potential prodrugs for anticancer therapy. Their activation via hydrolysis mechanisms was determined as a function of pH in buffer solutions, in human serum and in the presence of carboxyl ester hydrolase. Cytotoxicity was determined on various tumor cell lines and compared to the parent compound. On cell lines exhibiting resistance to etoposide we observed an enhanced cytotoxicity of the prodrugs of up to three orders of magnitude.
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pubmed:language |
eng
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pubmed:journal |
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pubmed:citationSubset |
IM
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pubmed:chemical |
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pubmed:status |
MEDLINE
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pubmed:month |
Feb
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pubmed:issn |
0960-894X
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pubmed:author |
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pubmed:issnType |
Print
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pubmed:day |
25
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pubmed:volume |
12
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
557-60
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pubmed:dateRevised |
2006-11-15
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pubmed:meshHeading |
pubmed-meshheading:11844671-Animals,
pubmed-meshheading:11844671-Antineoplastic Agents, Phytogenic,
pubmed-meshheading:11844671-Carboxylesterase,
pubmed-meshheading:11844671-Carboxylic Ester Hydrolases,
pubmed-meshheading:11844671-Cell Survival,
pubmed-meshheading:11844671-Esterases,
pubmed-meshheading:11844671-Etoposide,
pubmed-meshheading:11844671-Humans,
pubmed-meshheading:11844671-Hydrogen-Ion Concentration,
pubmed-meshheading:11844671-Hydrolysis,
pubmed-meshheading:11844671-Inhibitory Concentration 50,
pubmed-meshheading:11844671-Nucleic Acid Synthesis Inhibitors,
pubmed-meshheading:11844671-Prodrugs,
pubmed-meshheading:11844671-Swine,
pubmed-meshheading:11844671-Tumor Cells, Cultured
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pubmed:year |
2002
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pubmed:articleTitle |
Synthesis, hydrolytic activation and cytotoxicity of etoposide prodrugs.
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pubmed:affiliation |
Charité Children's Hospital, Humboldt University, Augustenburger Platz 1, 13353 Berlin, Germany. wrasidlo@charite.de
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pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
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