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Fluorinated tranylcypromine analogues as inhibitors of lysine-specific deme-thylase 1 (LSD1, KDM1A

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

Item Type: Article


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

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Uncontrolled Keywords: Organofluorine compounds Epigenetics FAD-dependent enzymes Lysine demethylase Mechanism based inhibitors
Depositing User: Teresa Borrello


Item ID: 15995
Identification Number:
ISSN: 0960-894X
Official URL:

Users with ORCIDS

ORCID for Maria Teresa Borrello: ORCID iD

Catalogue record

Date Deposited: 18 Sep 2023 08:54
Last Modified: 18 Sep 2023 08:54


Author: Maria Teresa Borrello ORCID iD
Author: Benjamin Schinor
Author: Katharina Bartels
Author: Hanae Benelkebir
Author: Sara Pereira
Author: Wafa T Al-Jamal
Author: Leon Douglas
Author: Patrick J Duriez
Author: Graham Packham
Author: Gunter Haufe
Author: A Ganesan

University Divisions

Faculty of Health Sciences and Wellbeing > School of Pharmacy and Pharmaceutical Sciences


Sciences > Chemistry
Sciences > Pharmacy and Pharmacology

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