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Issue 36, 2016
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C–H activation enables a rapid structure–activity relationship study of arylcyclopropyl amines for potent and selective LSD1 inhibitors

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Abstract

We describe the structure–activity relationship of various arylcyclopropylamines (ACPAs), which are potent LSD1 inhibitors. More than 45 ACPAs were synthesized rapidly by an unconventional method that we have recently developed, consisting of a C–H borylation and cross-coupling sequence starting from cyclopropylamine. We also generated NCD38 derivatives, which are known as LSD1 selective inhibitors, and discovered a more effective inhibitor compared to the original NCD38.

Graphical abstract: C–H activation enables a rapid structure–activity relationship study of arylcyclopropyl amines for potent and selective LSD1 inhibitors

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Publication details

The article was received on 12 Jul 2016, accepted on 13 Aug 2016 and first published on 15 Aug 2016


Article type: Paper
DOI: 10.1039/C6OB01483F
Citation: Org. Biomol. Chem., 2016,14, 8576-8585
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    C–H activation enables a rapid structure–activity relationship study of arylcyclopropyl amines for potent and selective LSD1 inhibitors

    S. Miyamura, M. Araki, Y. Ota, Y. Itoh, S. Yasuda, M. Masuda, T. Taniguchi, Y. Sowa, T. Sakai, T. Suzuki, K. Itami and J. Yamaguchi, Org. Biomol. Chem., 2016, 14, 8576
    DOI: 10.1039/C6OB01483F

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