Significant differences in biological parameters between prodrugs cleavable by carboxypeptidase G2 that generate 3, 5-difluoro-phenol and-aniline nitrogen mustards …

…, D Niculescu-Duvaz, F Friedlos, J Martin…

Index: Niculescu-Duvaz, Dan; Niculescu-Duvaz, Ion; Friedlos, Frank; Martin, Janet; Spooner, Robert; Davies, Lawrence; Marais, Richard; Springer, Caroline J. Journal of Medicinal Chemistry, 1998 , vol. 41, # 26 p. 5297 - 5309

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Citation Number: 29

Abstract

Nine new nitrogen mustard compounds derived from 2, 6-difluoro-4-hydroxy-(3a-e) and 2, 6- difluoro-4-amino-(4a-d) aniline were synthesized as potential prodrugs. They were designed to be activated to their corresponding 3, 5-difluorophenol and-aniline (4)-nitrogen mustards by the enzyme carboxypeptidase G2 (CPG2) in gene-directed enzyme prodrug therapy (GDEPT) models. The compounds were tested for cytotoxicity in the MDA MB-361 breast ...