A new method for rapidly generating inhibitors of glyoxalase I inside tumor cells using S-(N-aryl-N-hydroxycarbamoyl) ethylsulfoxides

DS Hamilton, MJ Kavarana, EM Sharkey…

Index: Hamilton, Diana S.; Kavarana, Malcolm J.; Sharkey, Ellyn M.; Eiseman, Julie L.; Creighton, Donald J. Journal of Medicinal Chemistry, 1999 , vol. 42, # 10 p. 1823 - 1827

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Citation Number: 15

Abstract

The enediol analogue S-(Np-chlorophenyl-N-hydroxycarbamoyl) glutathione is a powerful mechanism-based competitive inhibitor of the anticancer target enzyme glyoxalase I. Nevertheless, this compound exhibits limited toxicity toward tumor cells in vitro because it does not readily diffuse across cell membranes. We describe an efficient method for indirectly delivering the enzyme inhibitor into murine leukemia L1210 cells via acyl ...