59820-64-3Relevant articles and documents
Discovery of carbazole derivatives as novel allosteric MEK inhibitors by pharmacophore modeling and virtual screening
Xi, Dandan,Niu, Yan,Li, Hongyue,Noha, Stefan M.,Temml, Veronika,Schuster, Daniela,Wang, Chao,Xu, Fengrong,Xu, Ping
, p. 802 - 817 (2019/06/27)
We report in this work the discovery of novel allosteric MEK inhibitors by pharmacophore modeling and virtual screening. Two out of 13 virtual hit compounds were identified as MEK kinase inhibitors using a MEK1 binding assay. Structural derivations on the
Easy conjugations between molecules via copper-catalyzed reactions of ortho-aromatic diamines with ketones
Lu, Juyou,Yang, Haijun,Jin, Yunhe,Jiang, Yuyang,Fu, Hua
, p. 3184 - 3187 (2013/11/06)
It is a great challenge to achieve a useful reaction under benign conditions. In this paper, a highly efficient method for copper-catalyzed conjugations of o-aromatic diamines with ketones has been developed using benign chemistry. Interestingly, the conjugation between the biological small molecules worked very well.
Synthesis and biological activity of novel 1,2-disubstituted benzene derivatives as factor Xa inhibitors
Koshio, Hiroyuki,Hirayama, Fukushi,Ishihara, Tsukasa,Shiraki, Ryouta,Shigenaga, Takeshi,Taniuchi, Yuta,Sato, Kazuo,Moritani, Yumiko,Iwatsuki, Yoshiyuki,Kaku, Seiji,Katayama, Naoko,Kawasaki, Tomihisa,Matsumoto, Yuzo,Sakamoto, Shuichi,Tsukamoto, Shin-Ichi
, p. 1305 - 1323 (2007/10/03)
Factor Xa (fXa) is a serine protease that plays a pivotal role in the coagulation cascade. High-throughput screening of the Yamanouchi compound library yielded lead compound 1 with the ability to inhibit fXa at micromolar concentrations. To improve its fX
