5-Methoxyquinoline Derivatives as a New Class of EZH2 Inhibitors
AbstractA series of quinoline derivatives was synthesized and biologically evaluated as Enhancer of Zeste Homologue 2 (EZH2) inhibitors. Structure-activity relationship (SAR) studies led to the discovery of 5-methoxy-2-(4-methyl-1,4-diazepan-1-yl)-N-(1-methylpiperidin-4-yl)quinolin-4-amine (5k), which displayed an IC50 value of 1.2 μM against EZH2, decreased global H3K27me3 level in cells and also showed good anti-viability activities against two tumor cell lines. Due to the low molecular weight and the fact that no quinoline derivative has been reported as an EZH2 inhibitor, this compound could serve as a lead compound for further optimization. View Full-Text
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Xiang, P.; Jie, H.; Zhou, Y.; Yang, B.; Wang, H.-J.; Hu, J.; Hu, J.; Yang, S.-Y.; Zhao, Y.-L. 5-Methoxyquinoline Derivatives as a New Class of EZH2 Inhibitors. Molecules 2015, 20, 7620-7636.
Xiang P, Jie H, Zhou Y, Yang B, Wang H-J, Hu J, Hu J, Yang S-Y, Zhao Y-L. 5-Methoxyquinoline Derivatives as a New Class of EZH2 Inhibitors. Molecules. 2015; 20(5):7620-7636.Chicago/Turabian Style
Xiang, Pu; Jie, Hui; Zhou, Yang; Yang, Bo; Wang, Hui-Juan; Hu, Jing; Hu, Jian; Yang, Sheng-Yong; Zhao, Ying-Lan. 2015. "5-Methoxyquinoline Derivatives as a New Class of EZH2 Inhibitors." Molecules 20, no. 5: 7620-7636.