192997-46-9Relevant academic research and scientific papers
Discovery and optimization of selective FGFR4 inhibitors via scaffold hopping
Wang, Yikai,Chen, Zhengxia,Dai, Meibi,Sun, Peipei,Wang, Chunqiu,Gao, Yang,Zhao, Haixia,Zeng, Wenqin,Shen, Liang,Mao, Weifeng,Wang, Tian,Hu, Guoping,Li, Jian,Chen, Shuhui,Long, Chaofeng,Chen, Xiaoxin,Liu, Junhua,Zhang, Yang
supporting information, p. 2420 - 2423 (2017/05/10)
Introduction of a Michael acceptor on a flexible scaffold derived from pan-FGFR inhibitors has successfully yielded a novel series of highly potent FGFR4 inhibitors with selectivity over FGFR1. Due to reduced lipophilicity and aromatic ring count, this series demonstrated improved solubility and permeability. However, plasma instability and fast metabolism limited its potential for in vivo studies. Efforts have been made to address these problems, which led to the discovery of compound (?)-11 with improved stability, CYP inhibition, and good activity/selectivity for further optimization.
Self-assembly of dinuclear helical and nonhelical complexes with copper(I)
Rüttimann, Stéphane,Piguet, Claude,Bernardinelli, Gérald,Bocquet, Bernard,Williams, Alan F.
, p. 4230 - 4237 (2007/10/02)
The ligand 1,3-bis(1-methylbenzimidazol-2-yl)benzene (mbzimbe, L3) reacts with copper(I) to give [Cu2(L3)2](ClO4)2. The crystal structure of this compound (Cu2C44H36N8Cl2O 8, a = 13.661 (1) ?, b = 19.829 (3) ?, c = 15.413 (2) ?, orthorhombic, Pbca, Z = 4) shows a dinuclear centrosymmetrical nonhelical structure in which each copper is linearly coordinated by a benzimidazole group of each ligand. The complex displays a weak intramolecular stacking interaction between the benzene groups. This complex can be considered as a stereoconformer of the double-helical complex [Cu2(L1)2](ClO4)2 (L1; 2,6-bis(1-methylbenzimidazol-2-yl)pyridine). Conductivity measurements and UV-visible spectra show that the dimeric structures are maintained in solution in polar aprotic solvents. 1H NMR measurements show that [Cu2(L1)2]2+ retains its helical structure in solution. Comparison of helical and nonhelical structures with those formed by Cu(I) with related ligands allows discussion of the factors favoring the formation of self-assembled dinuclear complexes.
