Discovery Of New Tranylcypromine Derivatives As Highly Potent Lsd1 Inhibitors
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS(2021)
Abstract
Tranylcypromine (TCP)-based structural modifications lead to the discovery of new LSD1 inhibitors, of which compounds 26b and 29b effectively inhibit LSD1 with the IC50 values of 17 and 11 nM, respectively and also show good selectivity over MAO-B. Mechanistic studies showed that compound 29b concentration-dependently induced H3K4me1/2 accumulation in LSD1 overexpressed MGC-803 cells and also inhibited metastasis of MGC803 cells. Collectively, both compounds could be promising lead compounds for further investigation.
MoreTranslated text
Key words
Histone demethylase, Tranylcypromine, LSD1 inhibitor, Gastric cancer
AI Read Science
Must-Reading Tree
Example
![](https://originalfileserver.aminer.cn/sys/aminer/pubs/mrt_preview.jpeg)
Generate MRT to find the research sequence of this paper
Chat Paper
Summary is being generated by the instructions you defined