C-H activation enables a rapid structure-activity relationship study of arylcyclopropyl amines for potent and selective LSD1 inhibitors

Shin Miyamura, Misaho Araki, Yosuke Ota, Yukihiro Itoh, Shusuke Yasuda, Mitsuharu Masuda, Tomoyuki Taniguchi, Yoshihiro Sowa, Toshiyuki Sakai, Takayoshi Suzuki, Kenichiro Itami, Junichiro Yamaguchi

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    19 Citations (Scopus)

    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.

    Original languageEnglish
    Pages (from-to)8576-8585
    Number of pages10
    JournalOrganic and Biomolecular Chemistry
    Volume14
    Issue number36
    DOIs
    Publication statusPublished - 2016

    ASJC Scopus subject areas

    • Biochemistry
    • Physical and Theoretical Chemistry
    • Organic Chemistry

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    Miyamura, S., Araki, M., Ota, Y., Itoh, Y., Yasuda, S., Masuda, M., Taniguchi, T., Sowa, Y., Sakai, T., Suzuki, T., Itami, K., & Yamaguchi, J. (2016). C-H activation enables a rapid structure-activity relationship study of arylcyclopropyl amines for potent and selective LSD1 inhibitors. Organic and Biomolecular Chemistry, 14(36), 8576-8585. https://doi.org/10.1039/c6ob01483f