C-H活化使得能够对芳基环丙基胺进行快速的构效关系研究，以寻找强效且选择性的LSD1抑制剂。
C-H activation enables a rapid structure-activity relationship study of arylcyclopropyl amines for potent and selective LSD1 inhibitors.
作者信息
Miyamura Shin, Araki Misaho, Ota Yosuke, Itoh Yukihiro, Yasuda Shusuke, Masuda Mitsuharu, Taniguchi Tomoyuki, Sowa Yoshihiro, Sakai Toshiyuki, Suzuki Takayoshi, Itami Kenichiro, Yamaguchi Junichiro
机构信息
Institute of Transformative Bio-Molecules (WPI-ITbM) and Graduate School of Science, Nagoya University, Chikusa, Nagoya, 464-8602, Japan.
出版信息
Org Biomol Chem. 2016 Sep 28;14(36):8576-85. doi: 10.1039/c6ob01483f. Epub 2016 Aug 22.
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.
我们描述了各种芳基环丙胺（ACPA）的构效关系，这些芳基环丙胺是有效的赖氨酸特异性去甲基化酶1（LSD1）抑制剂。我们最近开发了一种非常规方法，从环丙胺开始，通过碳氢键硼化和交叉偶联序列，快速合成了45种以上的ACPA。我们还制备了已知为LSD1选择性抑制剂的NCD38衍生物，并发现了一种比原始NCD38更有效的抑制剂。
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