Abstract Glutathione S-transferase P1-1 (GSTP1-1, EC 2.5. 1.18) is generally conceived to be an important player in the acquired resistance of tumor to anticancer agents, thus a series of quinolinoneacetic acid derivatives were synthesized and their inhibitory effects on GSTP- 1 were tested in this study. Interestingly, it was found that some compounds showed remarkable inhibitory effect on GSTP-1 activity. Furthermore, molecular docking study was ...