1539-15-7Relevant academic research and scientific papers
Novel oxadiazole analogues derived from ethacrynic acid: Design, synthesis, and structure - Activity relationships in inhibiting the activity of glutathione S-transferase P1-1 and cancer cell proliferation
Yang, Xinmei,Liu, Guyue,Li, Hongcai,Zhang, Yun,Song, Dandan,Li, Chunmin,Wang, Rui,Liu, Bo,Liang, Wen,Jing, Yongkui,Zhao, Guisen
experimental part, p. 1015 - 1022 (2010/08/06)
Ethacrynic acid (EA) is a glutathione S-transferase P1-1 (GST P1-1) inhibitor with weak antiproliferative ability in tumor cells. By use of the principle of bioisosterism, a series of novel EA oxadiazole analogues were designed and synthesized. The struct
The synthesis of α,β-unsaturated carbonyl derivatives with the ability to inhibit both glutathione S-transferase P1-1 activity and the proliferation of leukemia cells
Zhao, Guisen,Liu, Chuan,Wang, Rui,Song, Dandan,Wang, Xiaobing,Lou, Hongxiang,Jing, Yongkui
, p. 2701 - 2707 (2008/02/07)
Ethacrynic acid (EA), an α,β-unsaturated carbonyl compound, is a glutathione S-transferase P1-1 (GSTP1-1) inhibitor. Twenty-one novel EA derivatives have been synthesized. The effects of these compounds on GSTP1-1 activity and on the proliferation of human leukemia HL-60 cells have been determined. Compounds with a halogen substitution at the 3′-position of the aromatic ring have greater inhibitory effects on GSTP1-1 activity than those of compounds with a methyl substitution there. Compounds with substitutions at both the 2′- and 3′-positions of the aromatic ring have more antiproliferative ability than those with one substitution at 3′-position. Esterification of the carboxyl group appears to increase the antiproliferative ability.
