This invention pertains to certain enzyme (CPG2) activated self-immolative
nitrogen mustard prodrugs, which are useful in enzyme prodrug therapy
(EPT), such as ADEPT and GDEPT, for the treatment of proliferative
conditions, such as cancer, and which have the following formula:
##STR00001## wherein: R.sup.N is independently C.sub.1-7alkyl; X.sup.1
is independently --I, --Br, or --Cl; X.sup.2 is independently --I, --Br,
or --Cl; the group --N(CH.sub.2CH.sub.2X.sup.1)(CH.sub.2CH.sub.2X.sup.2)
is independently attached at the 2-position or at the 4-position; each
R.sup.G is independently --H or an ester substituent; n is independently
an integer from 0 to 4; each R.sup.P, if present, is independently a
phenyl substituent; m is independently an integer from 0 to 4; each
R.sup.M, if present, is independently a mustard substituent; and
pharmaceutically acceptable salts, solvates, amides, and esters thereof.
The present invention also pertains to pharmaceutical compositions
comprising such compounds; such compounds and compositions for use in
methods of treatment of the human or animal body by therapy; the use of
such compounds and compositions for the manufacture of medicaments for
the treatment of proliferative conditions; and the like.