MedChemComm p. 650 - 654 (2014)
Update date:2022-07-29
Topics:
Ye, Xian-Wei
Zheng, Yi-Chao
Duan, Ying-Chao
Wang, Meng-Meng
Yu, Bin
Ren, Jing-Li
Ma, Jin-Lian
Zhang, En
Liu, Hong-Min
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 μM, 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. This journal is the Partner Organisations 2014.
View Morezhuzhou zhongle chemical co. ltd.
Contact:+86-0731 28228409
Address:Zhuzhou, Hunan, China
Contact:+86-18911665361
Address:Gaoxin district JiNan, China
Huangshan Honghui Pharm Technology Co., Ltd.(expird)
website:http://www.honghuichem.com
Contact:18855958372
Address:Qingshan Wan No.1,Nanyuan Kou,SheXian Huangshan City,Anhui Province
Contact:86-310-8067016
Address:East Fuhua Road,Tiexi Chemical Industrial Estate,Hebei,China
Sichuan Mianzhu Ronghong Chemical Co.,LTd
Contact:8613981840544
Address:XINSHI INDUSTRY PARK,MIANZHU,SICHUAN,CHINA
Doi:10.1002/hlca.19920750815
(1992)Doi:10.1021/acs.orglett.6b02278
(2016)Doi:10.1021/jo962068w
(1997)Doi:10.1016/j.tetlet.2016.09.054
(2016)Doi:10.1007/BF00961497
(1990)Doi:10.1021/ja01233a024
(1944)