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

Ting Li, Guyue Liu, Hongcai Li, Xinmei Yang, Yongkui Jing, Guisen Zhao

School of Pharmaceutical Sciences, Shandong University, Jinan, Shandong 250012, PR China.

Bioorganic & medicinal chemistry 2012 Apr 1

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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 thiazole exhibited improvement over EA to inhibit GSTpi activity. Copyright © 2012 Elsevier Ltd. All rights reserved.

Citation

Ting Li, Guyue Liu, Hongcai Li, Xinmei Yang, Yongkui Jing, Guisen Zhao. The synthesis of ethacrynic acid thiazole derivatives as glutathione S-transferase pi inhibitors. Bioorganic & medicinal chemistry. 2012 Apr 1;20(7):2316-22