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Synthesis and evaluation of novel daunomycin-phosphate-sulfate -β-glucuronide and -β-glucoside prodrugs for application in adept |
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| Authors: | Ruben G G Leenders Hans W ScheerenPieter H J Houba Epie Boven Hidde J Haisma |
| Institution: | Department of Organic Chemistry, NSR-Center for Molecular Structure, Design and Synthesis, University of Nijmegen, Toernooiveld, 6525 ED, Nijmegen, The Netherlands Department of Medical Oncology, Free University Hospital, De Boelelaan 1117, 1081 HV, Amsterdam, The Netherlands |
| 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-β-glucuronide and -β-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. |
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