Design, synthesis and biological evaluation of [1,2,4]triazolo[1,5-a]pyrimidines as potent lysine specific demethylase 1 (LSD1/KDM1A) inhibitors

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• 作者：Shuai Wang^a ; ¹ ; Li-Jie Zhao^a ; ¹ ; Yi-Chao Zheng^a ; Dan-Dan Shen^a ; Er-Fei Miao^a ; Xue-Peng Qiao^a ; Li-Juan Zhao^a ; Ying Liu^a ; Ruilei Huang^b ; Bin Yu^a ; ^{zzuyubin@hotmail.com} ; Hong-Min Liu^a ; ^{liuhm@zzu.edu.cn}
• 关键词：[1 ; 2 ; 4]triazolo[1 ; 5-a]pyrimidine ; Cytotoxicity ; LSD1 inactivation ; Migration inhibition ; Docking studies
• 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：940-951
• 全文大小：2571 K
• 卷排序：125

文摘

A new series of [1,2,4]triazolo[1,5-a]pyrimidine-based analogs were designed and synthesized. Compound 5p inactivated LSD1 potently (IC50 = 154 nM). Docking studies were performed to rationalize the potency against LSD1. Compound 5p inhibited migration of MGC-803 and PC-9 cells. Compound 6l showed excellent growth inhibition toward MGC-803 and PC-9 cells.