Prodrugs of anthracycline antibiotics suited for tumor-specific activation

Anticancer Drug Des. 1995 Sep;10(6):441-50.

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

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Antibiotics, Antineoplastic / chemistry*
  • Antibiotics, Antineoplastic / toxicity
  • Doxorubicin / chemistry*
  • Galactosides / chemistry
  • Leukemia L1210
  • Prodrugs / chemistry*
  • Prodrugs / toxicity
  • Tumor Cells, Cultured
  • alpha-Galactosidase / metabolism

Substances

  • Antibiotics, Antineoplastic
  • Galactosides
  • Prodrugs
  • Doxorubicin
  • alpha-Galactosidase