Aromatic mustards and aziridines and pharmaceutical uses thereof

A pharmaceutical composition for use in treatment of a neoplastic disease state in a mammal, said composition comprising a pharmaceutically-acceptable carrier and an effective amount of a compound of the general formula (I) ##STR12## wherein M and M.sub.1 separately represent H, aziridinyl, N(Et)CH.sub.2 CH.sub.2 Y or N(CH.sub.2 CH.sub.2 Y).sub.2, where Y is Cl, Br, I or OSO.sub.2 Me;

• R and R.sub.1 separately represent up to three of H or CH.sub.2 Q, such that at least one of R and R.sub.1 is CH.sub.2 NMe.sub.2, where Q is H, Me, (CH.sub.2).sub.n NMe.sub.2, (CH.sub.2).sub.m NHc(.dbd.NH)NH.sub.2 and n.dbd.0,2-4 and m.dbd.2-4 with the proviso that n may only be 0 when R or R.sub.1 is --CH.sub.2 Q, and Q is --(CH.sub.2).sub.n NMe.sub.2 ;
• X represents CONH or NHCO;
• and A is ##STR13## wherein Z.dbd.H, CH.sub.2 Q, SO.sub.2 NHQ or CONHQ, where Q is H, Me, (CH.sub.2).sub.p NMe.sub.2, (CH.sub.2).sub.p NHc(.dbd.NH)NH.sub.2 and p=2 to 4, or an acid addition salt or N-oxide thereof.

A method for treatment of neoplastic disease state in a mammal, said method comprising administering to a mammal in need of such treatment a therapeutically effective amount of a compound of the general formula (I) ##STR14## wherein M and M.sub.1 separately represent H, aziridinyl, N(Et)CH.sub.2 CH.sub.2 Y or N(CH.sub.2 CH.sub.2 Y).sub.2, where Y is Cl, Br, I or OSO.sub.2 Me;

• R and R.sub.1 separately represent up to three of H or CH.sub.2 Q, such that at least one of R and R.sub.1 is CH.sub.2 NMe.sub.2, where Q is H, Me, (CH.sub.2).sub.n NMe.sub.2, (CH.sub.2).sub.m NHC(.dbd.NH)NH.sub.2 and n=0, 2-4 and m=2-4 with the proviso that n may only be 0 when R or R.sub.1 is --CH.sub.2 Q, and Q is --(CH.sub.2).sub.n NMe.sub.2 ;
• X represents CONH or NHCO;
• and A is ##STR15## wherein Z.dbd.H, CH.sub.2 Q, SO.sub.2 NHQ or CONHQ, where Q is H, Me, (CH.sub.2).sub.p NMe.sub.2, (CH.sub.2p NHC(.dbd.NH)NH.sub.2, and p=2 to 4, or an acid addition salt or N-oxide thereof.