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Molecules 2015, 20(5), 7620-7636;

5-Methoxyquinoline Derivatives as a New Class of EZH2 Inhibitors

State Key Laboratory of Biotherapy and Cancer Center, West China Hospital, Sichuan University, and Collaborative Innovation Center for Biotherapy, Chengdu 610041, China
West China School of Pharmacy, Sichuan University, Chengdu 610041, China
The Second Division of Hepatobiliary Surgery, Center of PLA, Center of General Surgery of PLA, General Hospital of Chengdu Military Region, Chengdu 610083, China
These authors contributed equally to this work.
Author to whom correspondence should be addressed.
Academic Editor: Jean Jacques Vanden Eynde
Received: 15 January 2015 / Revised: 16 April 2015 / Accepted: 20 April 2015 / Published: 27 April 2015
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A 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
Keywords: histone methyltransferase; Enhancer of Zeste Homologue 2 (EZH2); quinolines; anticancer activity histone methyltransferase; Enhancer of Zeste Homologue 2 (EZH2); quinolines; anticancer activity

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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.

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