Competitive inhibitors of glyoxalase I and method of generating such competitive inhibitors inside tumor cells

A compound having the structure ##STR5## wherein S* is S.dbd.O or O.dbd.S.dbd.O;

• R.sub.1 is Z.sub.1 or Ar.sub.1 ;
• R.sub.2 is independently Z.sub.1 or Ar.sub.1 ;
• wherein Z.sub.1 is optionally substituted with Z.sub.2 or Z.sub.3,
• Z.sub.2 is optionally substituted with Z.sub.3,
• Ar.sub.1 is optionally substituted with Z.sub.4 ;
• and wherein
• Z.sub.1 is a C.sub.1 -C.sub.9 straight or branched chain alkyl or alkenyl group;
• Z.sub.2 is C.sub.3 -C.sub.8 cycloalkyl or C.sub.5 -C.sub.7 cycloalkenyl;
• Z.sub.3 is C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkenyl, or hydroxyl;
• Z.sub.4 is halo, hydroxyl, nitro, trifluoromethyl, optionally branched C.sub.1 -C.sub.6 alkyl, optionally branched C.sub.1 -C.sub.6 alkenyl, C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.4 alkenyloxy, phenoxy, benzyloxy or amino;
• Ar.sub.1 is selected from the group consisting of 1- or 2-naphthyl, 2- or 3-indolyl, 2- or 3-furyl, 2-thiazolyl, 2- or 3-thienyl, 2-, 3-, or 4-pyridyl, and phenyl;
• or pharmaceutically acceptable salts or hydrates thereof.