| abstract |
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) are provided Is done. The phenelzine analogs disclosed by the present invention show potency and selectivity for LSD1 compared to the MAO and LSD2 enzymes, as well as large scale gene specific histone methylation alterations, some cancers Shows antiproliferative activity in cell lines and neuroprotection in response to oxidative stress. Accordingly, the phenelzine analogs disclosed by the present invention can be used to treat diseases, conditions or disorders associated with LSD1 and / or HDAC, including but not limited to cancer and neurodegenerative diseases. . |