1357298-75-9Relevant articles and documents
C-H activation enables a rapid structure-activity relationship study of arylcyclopropyl amines for potent and selective LSD1 inhibitors
Miyamura, Shin,Araki, Misaho,Ota, Yosuke,Itoh, Yukihiro,Yasuda, Shusuke,Masuda, Mitsuharu,Taniguchi, Tomoyuki,Sowa, Yoshihiro,Sakai, Toshiyuki,Suzuki, Takayoshi,Itami, Kenichiro,Yamaguchi, Junichiro
, p. 8576 - 8585 (2016)
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.