Glucuronide prodrugs of hydroxy compounds for antibody directed enzyme prodrug therapy (ADEPT): a phenol nitrogen mustard carbamate

F Schmidt, JC Florent, C Monneret, R Straub…

Index: Schmidt; Florent; Monneret; Straub; Czech; Gerken; Bosslet Bioorganic and Medicinal Chemistry Letters, 1997 , vol. 7, # 8 p. 1071 - 1076

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Citation Number: 37

Abstract

A prodrug consisting of a β-D-glucuronic acid linked to a self-immolative spacer (a N-(ortho- hydroxyphenyl)-N-methylcarbamate) and a phenolic nitrogen mustard was synthesised. As this prodrug was easily cleaved by a β-glucuronidase enzyme and displayed low cytotoxicity, it must be considered as appropriate for an ADEPT approach.

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