Abstract
The two novel prodrugs 4 and 11 have been prepared from tetra-O-acetyl-D-galactopyranose and doxorubicin in three and six steps, respectively. Their low cytotoxicity, high stability in plasma and, in the case of 11, efficient hydrolysis in the presence of alpha-galactosidase, fulfill preliminary conditions for their use in combination with monoclonal antibody-enzyme conjugates.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Animals
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Antibiotics, Antineoplastic / chemistry*
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Antibiotics, Antineoplastic / toxicity
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Doxorubicin / chemistry*
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Galactosides / chemistry
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Leukemia L1210
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Prodrugs / chemistry*
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Prodrugs / toxicity
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Tumor Cells, Cultured
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alpha-Galactosidase / metabolism
Substances
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Antibiotics, Antineoplastic
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Galactosides
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Prodrugs
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Doxorubicin
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alpha-Galactosidase