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Prodrugs of anthracycline antibiotics suited for tumor-specific activation.
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1995
Year
Pharmaceutical ScienceBioorganic ChemistryGlycobiologyPolysaccharideAntimicrobial ChemotherapyPharmaceutical ChemistryDrug ResistanceMedicinal ChemistryAnthracycline AntibioticsAnti-cancer AgentMonoclonal Antibody-enzyme ConjugatesBiochemistryDrug DevelopmentPharmacologyHigh StabilityNovel Prodrugs 4Natural SciencesMedicineDrug Discovery
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.