Abstract
The three new hydrophilic prodrugs 2, 3 and 4 have been prepared from methyl (4-hydroxymethyl-2-nitrophenyl 2,3,4-tri-O-acetyl-beta-D-glucopyranosid)uronate (5) and doxorubicin. Their low cytotoxicity, efficient release of doxorubicin after hydrolysis by beta-D-glucuronidase, and in the cases of 2 and 3 stability at pH 7.2 fulfil the preliminary requirement for their use in antibody-directed enzyme prodrug therapy or prodrug monotherapy.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Antibiotics, Antineoplastic / chemistry*
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Antibiotics, Antineoplastic / metabolism
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Antibiotics, Antineoplastic / pharmacology
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Chromatography, High Pressure Liquid
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Doxorubicin / chemistry*
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Doxorubicin / metabolism
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Doxorubicin / pharmacology
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Drug Screening Assays, Antitumor
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Drug Stability
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Hydrolysis
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Prodrugs / chemical synthesis*
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Prodrugs / metabolism
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Prodrugs / pharmacology
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Tumor Cells, Cultured / drug effects
Substances
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Antibiotics, Antineoplastic
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Prodrugs
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Doxorubicin