title: The synthesis of ethacrynic acid thiazole derivatives as glutathione S-transferase pi inhibitors.
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 thiazole exhibited improvement over EA to inhibit GSTpi activity.
authors.affiliation: School of Pharmaceutical Sciences, Shandong University, Jinan, Shandong 250012, PR China.
authors.forename: Ting
authors.initials: T
authors.lastname: Li
authors.forename: Guyue
authors.initials: G
authors.lastname: Liu
authors.forename: Hongcai
authors.initials: H
authors.lastname: Li
authors.forename: Xinmei
authors.initials: X
authors.lastname: Yang
authors.forename: Yongkui
authors.initials: Y
authors.lastname: Jing
authors.forename: Guisen
authors.initials: G
authors.lastname: Zhao
mesh_terms: D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D004976:Ethacrynic Acid / Q000737:chemistry*; D051549:Glutathione S-Transferase pi / Q000037:antagonists & inhibitors* / Q000378:metabolism; D006801:Humans; D013329:Structure-Activity Relationship; D013844:Thiazoles / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology
chemical_list: D004791:Enzyme Inhibitors; D013844:Thiazoles; D051549:Glutathione S-Transferase pi; D004976:Ethacrynic Acid