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

Authors
Journal
Bioorganic & Medicinal Chemistry Letters
0960-894X
Publisher
Elsevier
Publication Date
Volume
7
Issue
8
Identifiers
DOI: 10.1016/s0960-894x(97)00157-1
Disciplines
  • Biology

Abstract

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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