School of Pharmaceutical Sciences, Shandong University, Jinan, Shandong 250012, PR China.
Bioorg Med Chem. 2012 Apr 1;20(7):2316-22. doi: 10.1016/j.bmc.2012.02.011. Epub 2012 Feb 13.
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.
谷胱甘肽 S-转移酶 pi（GSTpi）是一种 II 相酶，可保护细胞免于死亡并解毒癌细胞中的化疗药物。乙叉羟酸（EA）是一种弱 GSTpi 抑制剂。对其结构进行修饰以提高 EA 抑制 GSTpi 活性的能力。设计并合成了 18 种 EA 噻唑衍生物。用杂环噻唑取代 EA 的羧基的化合物 9a、9b 和 9c 对 GSTpi 活性的抑制作用优于 EA。
