207798-38-7Relevant articles and documents
Design, synthesis, and biological evaluation of 5-aminotetrahydroquinoline-based LSD1 inhibitors acting on Asp375
Yan, Jiangkun,Gu, Yanting,Sun, Yixiang,Zhang, Ziheng,Zhang, Xiangyu,Wang, Xinran,Wu, Tianxiao,Zhao, Dongmei,Cheng, Maosheng
, (2021/05/17)
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 biochemical evaluation of novel 5-aminotetrahydroquinoline-based LSD1 inhibitors. Among them, compounds A6, A8, B1–B5, and C4 showed preferable inhibitory effects on LSD1, with IC50 = 0.19–0.82 μM. 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 molecular 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.
Tetrahydroquinoline derivative as well as preparation method and application thereof
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Paragraph 0099; 0105-0107, (2020/12/31)
The invention belongs to the field of drug synthesis, and provides a tetrahydroquinoline derivative shown as a general formula (I) and pharmaceutically acceptable salt, stereoisomers or prodrugs thereof, in which A, Ra, Rb, n, m and R are as described in
Thieno[3,2-b]pyrrole-5-carboxamides as New Reversible Inhibitors of Histone Lysine Demethylase KDM1A/LSD1. Part 2: Structure-Based Drug Design and Structure-Activity Relationship
Vianello, Paola,Sartori, Luca,Amigoni, Federica,Cappa, Anna,Fagá, Giovanni,Fattori, Raimondo,Legnaghi, Elena,Ciossani, Giuseppe,Mattevi, Andrea,Meroni, Giuseppe,Moretti, Loris,Cecatiello, Valentina,Pasqualato, Sebastiano,Romussi, Alessia,Thaler, Florian,Trifiró, Paolo,Villa, Manuela,Botrugno, Oronza A.,Dessanti, Paola,Minucci, Saverio,Vultaggio, Stefania,Zagarrí, Elisa,Varasi, Mario,Mercurio, Ciro
supporting information, p. 1693 - 1715 (2017/03/20)
The balance of methylation levels at histone H3 lysine 4 (H3K4) is regulated by KDM1A (LSD1). KDM1A is overexpressed in several tumor types, thus representing an emerging target for the development of novel cancer therapeutics. We have previously describe