Enantioselective synthesis of tranylcypromine analogues as lysine demethylase (LSD1) inhibitors |
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Authors: | Benelkebir Hanae Hodgkinson Christopher Duriez Patrick J Hayden Annette L Bulleid Rosemary A Crabb Simon J Packham Graham Ganesan A |
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Institution: | School of Chemistry, University of Southampton, Southampton SO17 1BJ, United Kingdom. |
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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. |
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