THE JOHNS HOPKINS UNIVERSITY;INTONATION RESEARCH LABORATORIES
发明人:
PHILIP COLE,SHONOI MING,POLINA PRUSEVICH,JAY KALIN,RAMAN BAKSHI
申请号：
US15124208
公开号：
US20170029366A1
申请日:
2015.03.09
申请国别(地区):
US
年份:
2017
代理人:
摘要：
A series of phenelzine analogs comprising a phenelzine scaffold linked to an aromatic moiety and their use as inhibitors of lysine-specific demethylase 1 (LSD1) and/or one or more histone deacetylases (HDACs) is provided. The presently disclosed phenelzine analogs exhibit potency and selectivity for LSD1 versus MAO and LSD2 enzymes and exhibit bulk, as well as, gene specific histone methylation changes, anti-proliferative activity in several cancer cell lines, and neuroprotection in response to oxidative stress. Accordingly, the presently disclosed phenelzine analogs can be used to treat diseases, conditions, or disorders related to LSD1 and/or HDACs, including, but not limited to, cancers and neurodegenerative diseases.
