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Quinolinoneacetic acid derivatives as novel glutathione S-transferase P1-1 inhibitors: insights into the interaction modes by molecular modeling |
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| Authors: | Jian Wang Shao-Jie Wang Dan-Dan Song Yong-Kui Jing Mao-Sheng Cheng |
| Institution: | 1. Key Laboratory of Structure-Based Drug Design & Discovery of Ministry of Education, School of Pharmaceutical Engineering, Shenyang Pharmaceutical University, Shenyang, 110016, People’s Republic of China 2. School of Life Sciences & Biopharmaceutical Sciences, Shenyang Pharmaceutical University, Shenyang, 110016, People’s Republic of China 3. Mount Sinai School of Medicine, One Gustave L. Levy Place, New York, NY, 10029, USA |
| 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 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. |
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