Synthesis, SAR and pharmacological characterization of novel anthraquinone cation compounds as potential anticancer agents

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• 作者：Yanyan Zheng ; Li Zhu ; Lulu Fan ; Wenna Zhao ; Jianlong Wang ; Xianxiao Hao ; Yunhui Zhu ; Xiufang Hu ; Yaofeng Yuan ; Jingwei Shao ; ^{shaojingwei@fzu.edu.cn} ; Wenfeng Wang ; ^{wangwf@fzu.edu.cn}
• 关键词：Quaternary ammonium salt ; Reactive oxygen species ; Anticancer activity ; Quinoid structure ; Synthesis
• 刊名：European Journal of Medicinal Chemistry
• 出版年：2017
• 出版时间：5 January 2017
• 年：2017
• 卷：125
• 期：Complete
• 页码：902-913
• 全文大小：1671 K
• 卷排序：125

文摘

Fifteen novel emodin derivatives were designed and synthesized. Compound 4a showed significant antiproliferative activity in vitro. Compound 4a induced apoptosis through caspase-3 and P53 activation. Compound 4a directly effected on mitochondrial by generating ROS and decreasing ΔΨm.