31067-32-0Relevant articles and documents
Proton conductive cationic nanoporous polymers based on smectic liquid crystal hydrogen-bonded heterodimers
Mulder, Dirk-Jan,Liang, Ting,Xu, Yifei,Ter Schiphorst, Jeroen,Scheres, Luc M. W.,Oosterlaken, Bernette M.,Borneman, Zandrie,Nijmeijer, Kitty,Schenning, Albertus P.H.J.
, p. 5018 - 5024 (2018)
The fabrication of a cationic nanoporous smectic liquid crystal network (LCN) based on hydrogen bonded heterodimers is presented. The method relies on a supramolecular complex made from a pyridyl bearing reactive mesogen hydrogen bonded to a non-reactive benzoic acid template. Upon addition of a cross-linker, a smectic liquid crystalline phase is obtained that can be fixed by photopolymerization. It was found that the lamellar structure was maintained after template removal when 25 wt% or more cross-linker was used, yielding a nanoporous LCN. After H3PO4 immobilization in the pores of the LCN, a cationic 2D nanoporous polymer is obtained showing high and anisotropic anhydrous proton conductivity.
Permeant fluorescent probes visualize the activation of sarm1 and uncover an antineurodegenerative drug candidate
Cai, Yang,Cao, Sheng,Du, Yang,Hou, Yun Nan,Huang, Ke,Lee, Chi-Sing,Lee, Hon Cheung,Li, Wan Hua,Wang, Qian Wen,Wang, Sujing,Xie, Xu Jie,Zhang, Hongmin,Zhao, Yong Juan,Zhao, Zhi Ying,Zhu, Wen Jie
, (2021/06/30)
SARM1 regulates axonal degeneration through its NAD-metabolizing activity and is a drug target for neurodegenerative disorders. We designed and synthesized fluorescent conjugates of styryl derivative with pyridine to serve as substrates of SARM1, which exhibited large red shifts after conversion. With the conjugates, SARM1 activation was visualized in live cells following elevation of endogenous NMN or treatment with a cell-permeant NMN-analog. In neurons, imaging documented mouse SARM1 activation preceded vincristine-induced axonal degeneration by hours. Library screening identified a derivative of nisoldipine (NSDP) as a covalent inhibitor of SARM1 that reacted with the cysteines, especially Cys311 in its ARM domain and blocked its NMN-activation, protecting axons from degeneration. The Cryo-EM structure showed that SARM1 was locked into an inactive conformation by the inhibitor, uncovering a potential neuroprotective mechanism of dihydropyridines.
Design, synthesis and biological evaluation of pyrimidine-based derivatives as VEGFR-2 tyrosine kinase inhibitors
Sun, Wuji,Hu, Shengquan,Fang, Shubiao,Yan, Hong
, p. 393 - 405 (2018/04/23)
Vascular endothelial growth factor receptor-2 (VEGFR-2) plays a crucial role in tumor angiogenesis, and inhibition of the VEGFR-2 signaling pathway has already become an attractive approach for cancer therapy. In this study, a novel pyrimidine-based derivative 7j was designed as lead compound, and three series of potent VEGFR-2 inhibitors were synthesized and biologically evaluated against A549 and HepG2 cell lines. Compounds 7d, 9s and 13n exhibited superior inhibitory activities against A549 cell with IC50 ranged from 9.19 to 13.17 μM and HepG2 cell with IC50 ranged from 11.94 to 18.21 μM compared to those of Pazopanib (IC50 = 21.18 and 36.66 μM). In addition, molecular docking study was performed to investigate the binding capacity and binding mode between target compounds and VEGFR-2.
Discovery of novel picolinamide-based derivatives as novel VEGFR-2 kinase inhibitors: Synthesis,: in vitro biological evaluation and molecular docking
Sun, Wuji,Fang, Shubiao,Yan, Hong
, p. 1054 - 1058 (2018/06/27)
Vascular endothelial growth factor receptor-2 (VEGFR-2) plays a crucial role in tumor angiogenesis, and inhibition of the VEGFR-2 signaling pathway has emerged as an attractive target for cancer therapy. In our effort, a novel series of picolinamide-based derivatives were designed and synthesized as potent and effective VEGFR-2 inhibitors. All the newly prepared compounds were evaluated in vitro for their antiproliferative activity against A549 and HepG2 cell lines. Among the new compounds, 8j and 8l exhibited better activity against both A549 and HepG2 cell lines. Molecular docking was performed to investigate the binding capacity and binding mode with VEGFR-2 (PDB code: 4ASD).
Preparation method and application of turn-on type mercury ion fluorescence probe
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Paragraph 0010; 0031; 0032, (2018/12/13)
The invention discloses a preparation method and application of a turn-on type mercury ion fluorescence probe. For the mercury ion fluorescence probe, the molecular formula is C21H18INO2S, and the preparation method comprises the following steps of (1) pe
