131844-46-7Relevant academic research and scientific papers
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
supporting information, p. 8576 - 8585 (2016/09/28)
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.
Novel trans-2-aryl-cyclopropylamine analogues as potent and selective dipeptidyl peptidase IV inhibitors
Tsai, Ting-Yueh,Hsu, Tsu,Chen, Chiung-Tong,Cheng, Jai-Hong,Yeh, Teng-Kuang,Chen, Xin,Huang, Chung-Yu,Chang, Chung-Nien,Yeh, Kai-Chia,Hsieh, Su-Huei,Chien, Chia-Hui,Chang, Yi-Wei,Huang, Chih-Hsiang,Huang, Yu-Wen,Huang, Chen-Lung,Wu, Ssu-Hui,Wang, Min-Hsien,Lu, Cheng-Tai,Chao, Yu-Sheng,Jiaang, Weir-Torn
experimental part, p. 2388 - 2399 (2009/09/05)
A series of trans-2-aryl-cyclopropylamine derived compounds were synthesized and evaluated their biological activities against DPP-IV. The structure-activity relationships (SAR) led to the discovery of novel series of DPP-IV inhibitors, having IC50 values of 100 nM with excellent selectivity over the closely related enzymes, DPP8, DPP-II and FAP. The studies identified a potent and selective DPP-IV inhibitor 24b, which exhibited the ability to both significantly inhibit plasma DPP-IV activity in rats and improve glucose tolerance in lean mice and diet induced obese mice.
