Synthesis and biological evaluation of coumarin-1,2,3-triazole-dithiocarbamate hybrids as potent LSD1 inhibitors

被引：84
|
作者：
Ye, Xian-Wei [1 ]
Zheng, Yi-Chao [1 ]
Duan, Ying-Chao [2 ]
Wang, Meng-Meng [1 ]
Yu, Bin [1 ]
Ren, Jing-Li [1 ]
Ma, Jin-Lian [1 ]
Zhang, En [1 ]
Liu, Hong-Min [1 ]
机构：
[1] Zhengzhou Univ, Sch Pharmaceut Sci, New Drug Res & Dev Ctr, Zhengzhou 450001, Peoples R China
[2] Xinxiang Med Univ, Sch Pharm, Xinxiang 453003, Peoples R China
来源：
MEDCHEMCOMM | 2014年 / 5卷 / 05期
基金：
中国博士后科学基金; 中国国家自然科学基金;
关键词：
STRUCTURAL INSIGHTS; DESIGN; DEMETHYLATION; ANALOGS; TARGET;
D O I：
10.1039/c4md00031e
中图分类号：
Q5 [生物化学]; Q7 [分子生物学];
学科分类号：
071010 ; 081704 ;
摘要：
Two series of coumarin-1,2,3-triazole-dithiocarbamate hybrids were designed, synthesized and evaluated for their inhibitory activity towards lysine specific demethylase 1 (LSD1). Compounds 8a, 8d-8f, 8i-8l presented potent activity against lysine specific demethylase 1. Among them, compound 8k showed potent and reversible inhibition against lysine specific demethylase 1 with an IC50 value of 0.39 mu M, which was 74-fold more potent than that of tranylcypromine (2-PCPA). Besides, compound 8k displayed excellent selectivity against lysine specific demethylase 1 without inhibition against monoamine oxidases (MAOs) A and B. Further investigation revealed that compound 8k was active at both recombinant and cell levels by upregulating the expression of H3K4me1, H3K4me2 and H3K9me2.
引用
收藏
页码：650 / 654
页数：5
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