Borrello, Maria Teresa, Schinor, Benjamin, Bartels, Katharina, Benelkebir, Hanae, Pereira, Sara, Al-Jamal, Wafa T, Douglas, Leon, Duriez, Patrick J, Packham, Graham, Haufe, Gunter and Ganesan, A (2017) Fluorinated tranylcypromine analogues as inhibitors of lysine-specific deme-thylase 1 (LSD1, KDM1A. Bioorganic and Medicinal Chemistry Letters, 27 (10). pp. 2099-2101. ISSN 0960-894X
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Abstract
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
| Item Type: | Article |
|---|---|
| Uncontrolled Keywords: | Organofluorine compounds Epigenetics FAD-dependent enzymes Lysine demethylase Mechanism based inhibitors |
| Depositing User: | Teresa Borrello |
| URI: | https://sure.sunderland.ac.uk/id/eprint/15995 |
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