Blog

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.

Related post

  1. C-H Arylation and Alkenylation o…
  2. Structurally uniform and atomica…
  3. Synthesis and Properties of Cycl…
  4. Late-Stage C-H Bond Arylation of…
  5. Thiophene-Fused π-Systems from D…
  6. Size-Selective Complexation and …
  7. Theoretical Elucidation of Poten…
  8. Stepwise Generation of Mono-, Di…

Twitter@Itami Lab

Itami Lab Facebook

Instagram@Itami Lab

最近の記事

Flickr@Itamilab

天池先輩からコーヒースープ伴夫妻からのお歳暮です!潤さん、宮村さん、ありがとうございます!!武藤さん、ビールありがとうございます!平賀大都わーいやなさん、あつしさん、ありがとうございます!!だいぶ前だけど、Stripes look #ootdHalloween lookラインを洗う時ですら格好良く。戸谷先生教育実習!imageけいしゅう、誕生日おめでとう!誕生日は英吉家!!3年生に名古屋ぼろ勝ちアピール中!!アリシア卒業おめでとう女子会!
PAGE TOP