Quinolinoneacetic acid derivatives as novel glutathione S-transferase P1-1 inhibitors: insights into the interaction modes by molecular modeling

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 conducted to provide the binding modes of quinolinoneacetic acid derivatives on GSTP1-1 activity. In summary, we present the discovery of a series of quinolinoneacetic acid compounds as inhibitors of GSTP1-1 and their interaction modes toward GSTP1-1 binding site.