Inhibition Properties of Some Pyrimidine Derivatives as Anticancer Agents on Glutathione S-Transferase

Abstract

INTRODUCTION: Glutathione S-transferase (GST; EC 2.5.1.18), which is a member of the family of transferase enzymes, is an enzyme that has a very important role in maintaining the internal and external balance of the body by catalyzing the first stage of the formation reactions. mercapturic acid, the end product of detoxification metabolism. In this study, it was aimed to investigate the in vitro inhibition effect of pyrimidine derivatives on the GST enzyme. METHODS: TThe GST enzyme was purified by affinity chromatography technique. It was determined that pyrimidine derivatives strongly inhibited the GST enzyme at µM level. IC50 and KI values were calculated for the derivative compounds. RESULTS: All of the compounds whose effect was examined showed a noncompetitive inhibition effect on the GST enzyme. Moreover, 4-amino-2-chloropyrimidine showed the most effective inhibitory effect with its noncompetitive inhibition type. DISCUSSION AND CONCLUSION: It can be considered that pyrimidine derivatives may be effective on GST. The findings from this study make several contributions to the literature.

Keywords

• pyrimidine
• enzyme
• inhibition.