S-(N-Aryl-N-hydroxycarbamoy1) glutathione derivatives are powerful competitive inhibitors of the anticancer target enzyme glyoxalase I. Indeed, the Np-bromophenyl derivative is the strongest inhibitor of the enzyme from human erythrocytes yet reported (Ki= 1.4 X 10-8 M). Structureactivity correlations indicate that the high affinities of the derivatives for both human and yeast glyoxalase I are due to the fact that the derivatives are hydrophobic analogs of ...
