F. Schmidt et al., GLUCURONIDE PRODRUGS OF HYDROXY COMPOUNDS FOR ANTIBODY-DIRECTED ENZYME PRODRUG THERAPY (ADEPT) - A PHENOL NITROGEN-MUSTARD CARBAMATE, Bioorganic & medicinal chemistry letters, 7(8), 1997, pp. 1071-1076
A prodrug consisting of a beta-D-glucuronic acid linked to a self-immo
lative spacer (a N-(orthohydroxyphenyl)-N-methylcarbamate) and a pheno
lic nitrogen mustard was synthesised. As this prodrug was easily cleav
ed by a beta-glucuronidase enzyme and displayed low cytotoxicity, it m
ust be considered as appropriate for an ADEPT approach. (C) 1997 Elsev
ier Science Ltd.