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.
|Number of pages||6|
|Journal||Bioorganic & Medicinal Chemistry Letters|
|Publication status||Published - 21-Dec-1995|
- BIOLOGICAL EVALUATION
- ADRIAMYCIN ANALOGS