Prodrugs of anthracyclines for use in antibody-directed enzyme prodrug therapy

…, B Renoux, S Andrianomenjanahary…

Index: Florent, Jean-Claude; Dong, Xia; Gaudel, Gilbert; Mitaku, Sofia; Monneret, Claude; Gesson, Jean-Pierre; Jacquesy, Jean-Claude; Mondon, Martine; Renoux, Brigitte; Andrianomenjanahary, Solo; Michel, Sylvie; Koch, Michel; Tillequin, Francois; Gerken, Manfred; Czech, Joerg; Straub, Rainer; Bosslet, Klaus Journal of Medicinal Chemistry, 1998 , vol. 41, # 19 p. 3572 - 3581

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Citation Number: 86

Abstract

A series of new prodrugs of daunorubicin and doxorubicin which are candidates for antibody- directed enzyme prodrug therapy (ADEPT) is reported. These compounds (25a, b, c and 32a, b, c) have been designed to generate cytotoxic drugs after activation with β- glucuronidase. As expected, recovery of the active drug was observed after enzymatic cleavage by Escherichia coli β-glucuronidase as well as by a fusion protein which has ...