Fluorinated tranylcypromine analogues as inhibitors of lysine-specific demethylase 1 (LSD1, KDM1A)
Fluorinated tranylcypromine analogues as inhibitors of lysine-specific demethylase 1 (LSD1, KDM1A)
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.
Journal Article
2099-2101
Borrello, Maria Teresa
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Schinor, Benjamin
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Bartels, Katharina
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Benelkebir, Hanae
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Pereira, Sara
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Al-Jamal, Wafa T.
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Douglas, Leon
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Duriez, Patrick J.
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Packham, Graham
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Haufe, Günter
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Ganesan, Anusha
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15 May 2017
Borrello, Maria Teresa
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Schinor, Benjamin
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Bartels, Katharina
36ac0559-4a3f-413c-b3eb-8711eadc14ab
Benelkebir, Hanae
fbfb761f-8f66-4729-b376-6a228b28f142
Pereira, Sara
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Al-Jamal, Wafa T.
12867ec2-bc37-49d9-a48e-ef65fff573c0
Douglas, Leon
049b5f33-6870-4773-ae34-663489b472ba
Duriez, Patrick J.
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Packham, Graham
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Haufe, Günter
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Ganesan, Anusha
8453180c-2d4a-4415-b675-192df230a7b9
Borrello, Maria Teresa, Schinor, Benjamin, Bartels, Katharina, Benelkebir, Hanae, Pereira, Sara, Al-Jamal, Wafa T., Douglas, Leon, Duriez, Patrick J., Packham, Graham, Haufe, Günter and Ganesan, Anusha
(2017)
Fluorinated tranylcypromine analogues as inhibitors of lysine-specific demethylase 1 (LSD1, KDM1A).
Bioorganic & Medicinal Chemistry Letters, 27 (10), .
(doi:10.1016/j.bmcl.2017.03.081).
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.
Text
BorrelloBMCL2017RevisedManuscript
- Accepted Manuscript
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Accepted/In Press date: 25 March 2017
e-pub ahead of print date: 29 March 2017
Published date: 15 May 2017
Keywords:
Journal Article
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Local EPrints ID: 413054
URI: http://eprints.soton.ac.uk/id/eprint/413054
PURE UUID: a0db558e-6f95-4ea7-914a-942ba4ab27e6
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Date deposited: 14 Aug 2017 16:30
Last modified: 16 Mar 2024 05:24
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Contributors
Author:
Maria Teresa Borrello
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:
Günter Haufe
Author:
Anusha Ganesan
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