C-H activation enables a rapid structure-activity relationship study of arylcyclopropyl amines for potent and selective LSD1 inhibitorsElectronic supplementary information (ESI) available. See DOI: 10.1039/c6ob01483f
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 fro...
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| creator | Miyamura, Shin Araki, Misaho Ota, Yosuke Itoh, Yukihiro Yasuda, Shusuke Masuda, Mitsuharu Taniguchi, Tomoyuki Sowa, Yoshihiro Sakai, Toshiyuki Suzuki, Takayoshi Itami, Kenichiro Yamaguchi, Junichiro |
| description | 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.
Potent and selective LSD1 inhibitors were synthesized rapidly by a C-H borylation and cross-coupling sequence. |
| doi_str_mv | 10.1039/c6ob01483f |
| format | Article |
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| title | C-H activation enables a rapid structure-activity relationship study of arylcyclopropyl amines for potent and selective LSD1 inhibitorsElectronic supplementary information (ESI) available. See DOI: 10.1039/c6ob01483f |
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