Yan, Jiangkun; Gu, Yanting; Sun, Yixiang; Zhang, Ziheng; Zhang, Xiangyu; Wang, Xinran; Wu, Tianxiao; Zhao, Dongmei; Cheng, Maosheng published their research in Archiv der Pharmazie (Weinheim, Germany) in 2021. The article was titled 《Design, synthesis, and biological evaluation of 5-aminotetrahydroquinoline-based LSD1 inhibitors acting on Asp375》.Recommanded Product: 109384-19-2 The article contains the following contents:
The abnormal expression of lysine-specific histone demethylase 1 (LSD1) is associated with different cancer types, and LSD1 inhibitory activity seems to have high therapeutic potential in cancer treatment. Here, we report the design, synthesis, and biochem. evaluation of novel 5-aminotetrahydroquinoline-based LSD1 inhibitors such as I. Among them, eight of the compounds showed preferable inhibitory effects on LSD1, with IC50 = 0.19-0.82μM. Several potent compounds were selected to evaluate their antiproliferative activity on A549 cells and MCF-7 cells with a high expression of LSD1. The potential binding modes of the compounds were revealed through mol. docking to rationalize the potency of compounds toward LSD1. Our data recognized that the 5-aminotetrahydroquinoline scaffold may serve as a starting point for developing potent LSD1 inhibitors for cancer therapy. In the experiment, the researchers used tert-Butyl 4-hydroxypiperidine-1-carboxylate(cas: 109384-19-2Recommanded Product: 109384-19-2)
tert-Butyl 4-hydroxypiperidine-1-carboxylate(cas:109384-19-2) is a 4-hydroxypyridine with a boc protecting group used in the preparation of neurologically active agents and other pharmaceutical compounds.Recommanded Product: 109384-19-2
Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem