Fluorinated tranylcypromine analogues as inhibitors of lysine-specific demethylase 1 (LSD1, KDM1A)

Maria Teresa Borrello, Benjamin Schinor, Katharina Bartels, Hanae Benelkebir, Sara Pereira, Wafa T Al-Jamal, Leon Douglas, Patrick J Duriez, Graham Packham, Günter Haufe, A Ganesan

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Abstract

We report a series of tranylcypromine analogues containing a fluorine in the cyclopropyl ring. A number of compounds with additional m- or p-substitution of the aryl ring were micromolar inhibitors of the LSD1 enzyme. In cellular assays, the compounds inhibited the proliferation of acute myeloid leukemia cell lines. Increased levels of the biomarkers H3K4me2 and CD86 were consistent with LSD1 target engagement.

Original languageEnglish
Pages (from-to)2099-2101
JournalBioorganic and Medicinal Chemistry Letters
Volume27
Issue number10
Early online date29 Mar 2017
DOIs
Publication statusPublished - 15 May 2017

Keywords

  • Journal Article

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    Borrello, M. T., Schinor, B., Bartels, K., Benelkebir, H., Pereira, S., Al-Jamal, W. T., Douglas, L., Duriez, P. J., Packham, G., Haufe, G., & Ganesan, A. (2017). Fluorinated tranylcypromine analogues as inhibitors of lysine-specific demethylase 1 (LSD1, KDM1A). Bioorganic and Medicinal Chemistry Letters, 27(10), 2099-2101. https://doi.org/10.1016/j.bmcl.2017.03.081