Synthesis of glutathione analogues and screening as substrates & inhibitors for human glutathione transferase p1‐1

Abstract

A major detoxification mechanism of the cell involves the glutathione transferase (GST)‐catalyzed formation of glutathione (GSH) conjugates with various xenobiotics Based on the same mechanism, GST overexpression may lead to multidrug resistant phenotypes Therefore, several compounds with inhibitory potency against GSTs have been developed as potential tools fortackling GST-­‐attributed MDR. Several individual compounds and prodrugs have been proposed as GST‐inhibiting substances. In addition, GSH analogues have been considered as specific GST inhibitors, with particular attention been directed towards the synthesis of GSH analogues stable against γ‐glutamyltranspeptidase (γGT) and peptidases, as GST inhibitors.