Benelkebir, Hanae, Hodgkinson, Christopher, Duriez, Patrick J., Hayden, Annette L., Bulleid, Rosemary A., Crabb, Simon J., Packham, Graham and Ganesan, A ORCID: https://orcid.org/0000-0003-4862-7999
(2011)
Enantioselective synthesis of tranylcypromine analogues as lysine demethylase (LSD1) inhibitors.
Bioorganic & Medicinal Chemistry, 19 (12).
pp. 3709-3716.
Abstract
Asymmetric cyclopropanation of styrenes by tert-butyl diazoacetate followed by ester hydrolysis and Curtius rearrangement gave a series of tranylcypromine analogues as single enantiomers. The o,- m- and p-bromo analogues were all more active than tranylcypromine in a LSD1 enzyme assay. The m- and p-bromo analogues were micromolar growth inhibitors of the LNCaP prostate cancer cell line as were the corresponding biphenyl analogues prepared from the bromide by Suzuki crosscoupling.
Item Type: | Article |
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Uncontrolled Keywords: | sdg 3 - good health and well-being ,/dk/atira/pure/sustainabledevelopmentgoals/good_health_and_well_being |
Faculty \ School: | Faculty of Science > School of Pharmacy |
Depositing User: | Users 2731 not found. |
Date Deposited: | 20 Oct 2011 10:36 |
Last Modified: | 22 Oct 2022 21:33 |
URI: | https://ueaeprints.uea.ac.uk/id/eprint/35102 |
DOI: | 10.1016/j.bmc.2011.02.017 |
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