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

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

  • Org Biomol Chem. 2016 Sep 28;14(36):8576-85. doi: 10.1039/c6ob01483f.
Shin Miyamura 1,  Misaho Araki,  Yosuke Ota,  Yukihiro Itoh,  Shusuke Yasuda,  Mitsuharu Masuda,  Tomoyuki Taniguchi,  Yoshihiro Sowa,  Toshiyuki Sakai,  Takayoshi Suzuki,  Kenichiro Itami,  Junichiro Yamaguchi
Affiliations

Affiliation

  • 1 Institute of Transformative Bio-Molecules (WPI-ITbM) and Graduate School of Science, Nagoya University, Chikusa, Nagoya, 464-8602, Japan.
PMID: 27548471 DOI: 10.1039/c6ob01483f
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.

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