Synthesis and evaluation of novel daunomycin-phosphate -sulfate -beta-glucuronide and -beta-glucoside prodrugs for application in ADEPT.

RGG Leenders, HW Scheeren, PHJ Houba, E Boven, HJ Haisma

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21 Citations (Scopus)

Abstract

The synthesis, antiproliferative effect and enzymatic hydrolysis of daunomycin-3'-N- and -4'-O-phosphate and -sulfate derivatives and of daunomycin-3'-N-CO-beta-glucuronide and -beta-glucoside, designed to be prodrugs in ADEPT are described. The phosphate derivatives were almost as toxic as the parent drug whereas the sulfates were not hydrolyzed by aryl sulfatases, Glucuronyl and glucosyl prodrugs were found to be useful for application in ADEPT.

Original languageEnglish
Pages (from-to)2975-2980
Number of pages6
JournalBioorganic & Medicinal Chemistry Letters
Volume5
Issue number24
Publication statusPublished - 21-Dec-1995

Keywords

  • BIOLOGICAL EVALUATION
  • ADRIAMYCIN ANALOGS
  • ANTIBODY
  • CONJUGATE
  • CANCER
  • COMBINATION
  • DERIVATIVES
  • ENZYMES
  • INVITRO

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