Novel anthracycline-spacer-β-glucuronide,-β-glucoside, and-β-galactoside prodrugs for application in selective chemotherapy

…, PHJ Houba, IH van der Meulen-Muileman…

Index: Leenders, Ruben G. G.; Damen, Eric W. P.; Bijsterveld, Edward J. A.; Scheeren, Hans W.; Houba, Pieter H. J.; Van Der Meulen-Muileman, Ida H.; Boven, Epie; Haisma, Hidde J. Bioorganic and Medicinal Chemistry, 1999 , vol. 7, # 8 p. 1597 - 1610

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Citation Number: 61

Abstract

A series of anthracycline prodrugs containing an immolative spacer was synthesized for application in selective chemotherapy. The prodrugs having the general structure anthracycline-spacer-β-glycoside were designed to be activated by β-glucuronidase or β- galactosidase. Prodrugs with-chloro,-bromo or-n-hexyl substituents on the spacer were synthesized as well as prodrugs containing a-β-glucuronyl,-β-glucosyl or-β-galactosyl ...