- Borane-Catalyzed Chemoselective and Enantioselective Reduction of 2-Vinyl-Substituted Pyridines
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Herein, we report that highly chemoselective and enantioselective reduction of 2-vinyl-substituted pyridines has been achieved for the first time. The reaction, which uses chiral spiro-bicyclic bisboranes as catalysts and HBpin and an acidic amide as reducing reagents, proceeds through a cascade process involving 1,4-hydroboration followed by transfer hydrogenation of a dihydropyridine intermediate. The retained double bond in the reduction products permits their conversion to natural products and other useful heterocyclic compounds by simple transformations.
- Hu, Chen-Yu,Li, Xiang,Liang, Xin-Shen,Liu, Ning,Tian, Jun-Jie,Tu, Xian-Shuang,Wang, Xiao-Chen,Yang, Zhao-Ying
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supporting information
p. 18452 - 18456
(2020/08/21)
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- Design, synthesis and biological evaluation of pyrimidine-based derivatives as VEGFR-2 tyrosine kinase inhibitors
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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.
- Sun, Wuji,Hu, Shengquan,Fang, Shubiao,Yan, Hong
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p. 393 - 405
(2018/04/23)
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- Discovery of novel picolinamide-based derivatives as novel VEGFR-2 kinase inhibitors: Synthesis,: in vitro biological evaluation and molecular docking
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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).
- Sun, Wuji,Fang, Shubiao,Yan, Hong
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supporting information
p. 1054 - 1058
(2018/06/27)
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- Synthesis of new conjugated polymers as hole injection layer and performance of OLED devices
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The fluorene-based poly(dioctylfluorene-alt-biphenylamine)s with styrylpyridyl group were synthesized by using Pd-catalyzed polycondensation reaction. These hole injection/ transport polymers showed very good solvent resistance after photo-crosslinking which could facilitate the subsequent spin coating of the emitting layer polymer solution. Moreover these polymers could be patterned by using distyrylpyridyl alkyl monomer (DSM) as crosslinking agents. The OLED devices with configuration of ITO/HIL/Alq3:NPD/LiF/Al in which synthesized polymer was used as hole injection layer (HIL) were fabricated and their performance was compared with the commercially available PEDOT:PSS as HIL layer.
- Yoo, Tae Wook,Park, Chul,Mai, Nguyen Thi,Kim, Dong Uk,Park, Lee Soon
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scheme or table
p. 69 - 77
(2012/05/04)
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- Comparative syntheses of arylamine monomer with styrylpyridyl photo-crosslinker of polyarylamine for OLED hole-injection material
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A new arylamine monomer with photo-crosslinkable styrylpyridinyl moiety of conjugated polyarylamine for OLED hole injection material was synthesized through two synthetic routes, BOC-amine protection/deprotection and nitro group reduction methods. Both sy
- Choi, Heung-Jin,Song, Moo-Gon,Sim, Youn-Hee,Bae, Heung-Kwon,Kim, Jin-Woo,Park, Lee Soon
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experimental part
p. 47 - 54
(2011/08/02)
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- Synthesis and photolithographic property of conjugated polymers with polyazomethine structure
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Two different polyazomethine-type conjugated polymers, poly(phenoxiazine-3, 3′-dihydroxybensidine)(PZ-DHB) and poly(phenoxiazine-2,4-diamino-6- hydroxypyrimidine)(PZ-DHP) containing phenothiazine moiety and azomethine linkage in the main chain were synthe
- Ryu, Sang Chul,Jeong, Young Chul,Park, Lee Soon
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experimental part
p. 235 - 248
(2010/07/14)
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