The synthesis of ethacrynic acid thiazole derivatives as glutathione S-transferase pi inhibitors
作者:Ting Li、Guyue Liu、Hongcai Li、Xinmei Yang、Yongkui Jing、Guisen Zhao
DOI:10.1016/j.bmc.2012.02.011
日期:2012.4
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II期酶,可保护细胞免于死亡,并清除癌细胞中的化学治疗剂。乙炔酸(EA)是一种弱的GSTpi抑制剂。进行结构修饰以提高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显示出相对于EA的改善,以抑制GSTpi活性。