Discovery of new tranylcypromine derivatives as highly potent LSD1 inhibitors

[Display omitted] 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 c...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2021-06, Vol.41, p.127993-127993, Article 127993
Hauptverfasser:	Huang, Ming-Jie, Guo, Jia-Wen, Fu, Yun-Dong, You, Ya-Zhen, Xu, Wen-Yu, Song, Ting-Yu, Li, Ran, Chen, Zi-Tong, Huang, Li-Hua, Liu, Hong-Min
Format:	Artikel
Sprache:	eng
Schlagworte:	Gastric cancer Histone demethylase LSD1 inhibitor Tranylcypromine
Online-Zugang:	Volltext
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