A β-galactoside phosphoramide mustard prodrug for use in conjunction with gene-directed enzyme prodrug therapy
Abstract
4-(β-D-Galactopyranosyl)benzyl N,N,N′,N′-tetrakis(2-chloroethyl)phosphorodiamidate 1 was facilely biotransformed to the alkylating antitumor agent, N,N,N′,N′-tetrakis(2-chloroethyl) phosphorodiamidic acid, 4, when incubated with E. coli β-galactosidase, and therefore has potential for use in conjunction with gene-directed enzyme prodrug therapy.