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

*この研究の対応する著者

研究成果: Article査読

24 被引用数 (Scopus)

抄録

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.

本文言語English
ページ(範囲)8576-8585
ページ数10
ジャーナルOrganic and Biomolecular Chemistry
14
36
DOI
出版ステータスPublished - 2016

ASJC Scopus subject areas

  • 生化学
  • 物理化学および理論化学
  • 有機化学

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