321337-38-6Relevant 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.
TRICYCLIC DEGRADERS OF IKAROS AND AIOLOS
-
, (2020/10/21)
Tricyclic cereblon binders for the degradation of Ikaros or Aiolos by the ubiquitin proteasome pathway for therapeutic applications are described.
Benzodiazepine derivatives
-
, (2008/06/13)
The present invention provides benzodiazepine derivatives of the following formula, analogs thereof and pharmaceutically acceptable salts thereof. The compounds of the present invention have an excellent effect of inhibiting activated blood-coagulation factor X. These compounds are usable as agents for treating various diseases concerned with the activated blood-coagulation factor X.