Discovery of resveratrol derivatives as novel LSD1 inhibitors: Design, synthesis and their biological evaluation

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• 作者：Ying-Chao Duan^a ; Yuan-Yuan Guan^b ; Xiao-Yu Zhai^a ; Li-Na Ding^c ; Wen-Ping Qin^a ; Dan-Dan Shen^c ; Xue-Qi Liu^c ; Xu-Dong Sun^c ; Yi-Chao Zheng^c ; ^{yichaozheng@zzu.edu.cn} ; Hong-Min Liu^c ; ^{liuhm@zzu.edu.cn}
• 关键词：Lysine-specific demethylase 1 inhibitors ; Resveratrol derivatives ; Synthesis
• 刊名：European Journal of Medicinal Chemistry
• 出版年：2017
• 出版时间：27 January 2017
• 年：2017
• 卷：126
• 期：Complete
• 页码：246-258
• 全文大小：2091 K
• 卷排序：126

文摘

A series of resveratrol derivatives were discovered as novel LSD1 inhibitors. Most compounds exhibited potent inhibitory activities against recombinant LSD1. Compounds 4e and 4m elevated the level of H3K4Me2 significantly in MGC-803 cells. Compounds 4e and 4m increased the expression level of CD86 mRNA in MGC-803 cells.