- Discovery of carbazole derivatives as novel allosteric MEK inhibitors by pharmacophore modeling and virtual screening
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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
- Xi, Dandan,Niu, Yan,Li, Hongyue,Noha, Stefan M.,Temml, Veronika,Schuster, Daniela,Wang, Chao,Xu, Fengrong,Xu, Ping
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p. 802 - 817
(2019/06/27)
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- Novel aromatic sulfonyl naphthalene-based boronates as 20S proteasome inhibitors
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A novel series of non-peptide proteasome inhibitors (PIs) that act on chymotrypsin-like (ChT-L) of the proteasome were developed. These PIs bearing 4-aromatic sulfonyl naphthalene-based scaffold and Leu-boronic moiety as covalent bonding group displayed f
- Liu, Hongwu,Wu, Jianwei,Ge, Ying,Li, Aibo,Li, Jia,Liu, Zhengshi,Xu, Yungen,Xu, Qingxiang,Li, Yuyan
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p. 1050 - 1061
(2018/02/19)
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- Some reactions of new semiquinoid compounds derived from N-arylsulfonyl-p-quinonimines
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Polyhalogenated semiquinoid compounds on the basis of N-arylsulfonyl-p-quinonimines react with reducing agents (zinc or sodium dithionite in acetic acid) with elimination of one or two hydrogen halide molecules, depending on the number of hydrogens at the sp3-hybridized carbon atoms, to give the corresponding benzoid structures. Dehydrohalogenation of the title compounds in chloroform in the presence of triethylamine leads to formation of quinonimines. N,N′-Bis(arylsulfonyl)-p-quinonediimine derivatives do not undergo dehydrohalogenation. Reactions with dialkyl hydrogen phosphites result mostly in 1,2-addition and formation of phosphorylated products; the reaction is likely to involve intermediate dehydrohalogenation to the corresponding quinonimines which can be isolated in the pure state.
- Avdeenko,Zhukova
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p. 1482 - 1489
(2007/10/03)
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- CHLORINATION OF N-ARYLSULFONYL-1,4-AMINONAPHTHOLS AND N-ARYLSULFONYL-1,4-NAPHTHOQUINONE 4-IMINES
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The final products from the chlorination of N-arylsulfonyl-1,4-aminonaphthols and N-arylsulfonyl-1,4-naphthoquinone 4-imines are 4-arylsulfonylimino-1-oxo-2,2,3,3,-tetrachloro-1,2,3,4-tetrahydronaphthalenes.
- Avdeenko, A. P.,Velichko, N. V.,Romanenko, E. A.,Pirozhenko, V. V.
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p. 1535 - 1543
(2007/10/02)
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