Bioorganic & medicinal chemistry

The synthesis of ethacrynic acid thiazole derivatives as glutathione S-transferase pi inhibitors

T Li, G Liu, H Li, X Yang, Y Jing, G Zhao

Index: Li, Ting; Liu, Guyue; Li, Hongcai; Yang, Xinmei; Jing, Yongkui; Zhao, Guisen Bioorganic and Medicinal Chemistry, 2012 , vol. 20, # 7 p. 2316 - 2322

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Citation Number: 8

Abstract

Glutathione S-transferase pi (GSTpi) is a phase II enzyme which protects cells from death and detoxifies chemotherapeutic agents in cancer cells. Ethacrynic acid (EA) is a weak GSTpi inhibitor. Structure modifications were done to improve the ability of EA to inhibit GSTpi activity. Eighteen EA thiazole derivatives were designed and synthesized. Compounds 9a, 9b and 9c with a replacement of carboxyl group of EA by a heterocyclic ...