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C-H Activation Enables Rapid Structure-Activity Relationship Study of Arylcyclopropyl amines for Potent and Selective LSD1 Inhibitors

Miyamura, S.; Araki, M; Ota, Y; Itoh, Y; Yasuda, S; Masada, M; Taniguchi, T; Sowa, Y; Sakai, T; Suzuki, T;* Itami, K*; Yamaguchi, J*

Org. Biomol. Chem.  2016, Accepted Manuscripts 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 from cyclopropylamine.[1] We also generated NCD38 derivatives, which are known as LSD1 selective inhibitors, and discovered a more effective inhibitor compared to the original NCD38.

[1] Miyamura, S.; Araki, M.; Suzuki, T.; Yamaguchi, J.; Itami, K. Angew. Chem., Int. Ed201554, 846.

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