61248-99-5Relevant articles and documents
A low toxic CRM1 degrader: Synthesis and anti-proliferation on MGC803 and HGC27
Jia, Shilong,Jin, Cheng-Yun,Li, Xiaobo,Liu, Mengbo,Meng, Xia,Wang, Menglin,Wu, Xinxin,Xu, Hai-Wei,Yu, Lu
, (2020/08/19)
Chromosome region maintenance 1 (CRM1) is the sole nuclear exporter of several tumor suppressor, a growth regulatory protein as an attractive cancer drug target. In the present work, a novel CRM1 degrader was discovered from newly synthesized α, β-unsaturated-δ-lactone based on a natural product Goniothalamin. It induces apoptosis of both MGC803 and HGC27 cell lines via degrading CRM1. Selective inhibition was observed for the proliferation of gastric cancer cell lines MGC803, HGC27 comparing to Human Gastric Mucosal Epithelial Cell Line (GES1). For the first time, CRM1 inhibitor or degrader inducing apoptosis in gastric carcinoma was investigated.
Chiral Bifunctional Metalloporphyrin Catalysts for Kinetic Resolution of Epoxides with Carbon Dioxide
Maeda, Chihiro,Mitsuzane, Mayato,Ema, Tadashi
supporting information, p. 1853 - 1856 (2019/03/11)
Chiral binaphthyl-strapped Zn(II) porphyrins with triazolium halide units were synthesized as bifunctional catalysts for kinetic resolution of epoxides with CO2. Several catalysts were screened by changing the linker length and nucleophilic counteranions, and the optimized catalyst accelerated the enantioselective reaction at ambient temperature to produce optically active cyclic carbonates and epoxides.
Chiral Macrocyclic Organocatalysts for Kinetic Resolution of Disubstituted Epoxides with Carbon Dioxide
Ema, Tadashi,Yokoyama, Maki,Watanabe, Sagiri,Sasaki, Sota,Ota, Hiromi,Takaishi, Kazuto
supporting information, p. 4070 - 4073 (2017/08/15)
Among chiral macrocycles 1 synthesized, 1m with the 3,5-bis(trifluoromethyl)phenylethynyl group was the best organocatalyst for the enantioselective synthesis of cyclic carbonates from disubstituted or monosubstituted epoxides and CO2. The X-ray crystal structure of 1m revealed a well-defined chiral cavity with multiple hydrogen-bonding sites that is suitable for the enantioselective activation of epoxides. A catalytic cycle proposed was supported by DFT calculations.