Fluorinated tranylcypromine analogues as inhibitors of lysine-specific demethylase 1 (LSD1, KDM1A)
作者： Maria Teresa Borrello , Benjamin Schinor , Katharina Bartels , Hanae Benelkebir , Sara Pereira
DOI: 10.1016/J.BMCL.2017.03.081
关键词:
摘要: We report a series of tranylcypromine analogues containing fluorine in the cyclopropyl ring. A number compounds with additional m- or p-substitution aryl ring were micromolar inhibitors LSD1 enzyme. In cellular assays, inhibited proliferation acute myeloid leukemia cell lines. Increased levels biomarkers H3K4me2 and CD86 consistent target engagement.
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