The glyoxalase enzymes represent a cellular defence system against the accumulation of cytotoxic α-oxoaldehydes leading to apoptosis. The potential of glyoxalase inhibitors to act as novel anti-cancer agents for drugresistant tumours that over-express glyoxalase is currently under investigation. In the present study, a series of 6-sulfamoylsaccharin and 1, 2- benzoxathiine 2, 2-dioxide (sulfocoumarin-coumarin bioisostere) derivates, as well as, ...