- Structure-based design and profiling of novel 17β-HSD14 inhibitors
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The human enzyme 17β-hydroxysteroid dehydrogenase 14 (17β-HSD14) oxidizes the hydroxyl group at position 17 of estradiol and 5-androstenediol using NAD+ as cofactor. However, the physiological role of the enzyme remains unclear. We recently des
- Braun, Florian,Bertoletti, Nicole,M?ller, Gabriele,Adamski, Jerzy,Frotscher, Martin,Guragossian, Nathalie,Madeira Gírio, Patrícia Alexandra,Le Borgne, Marc,Ettouati, Laurent,Falson, Pierre,Müller, Sebastian,Vollmer, Günther,Heine, Andreas,Klebe, Gerhard,Marchais-Oberwinkler, Sandrine
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supporting information
p. 61 - 76
(2018/06/01)
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- Quinoline derivatives and their use
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The invention discloses a quinoline derivative and a usage thereof, a compound with a structure as shown in a formula (I) and or a pharmaceutically acceptable salt of the compound. The compound or the pharmaceutically acceptable salt thereof disclosed by the invention can be applied to the field of preparation of drugs for preventing or treating tumors.
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Paragraph 0099-0101; 0168; 0169; 0186; 0187
(2017/03/14)
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- A highly practical and convenient halogenation of fused heterocyclic N-oxides
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A novel, simple and practical method for the regioselective halogenation of fused heterocyclic N-oxides has been developed. It employs Vilsmeier reagent, generated in situ by POX3and DMF, as both the activating agent and the nucleophilic halide source. The method is amenable across a broad range of substrates, including quinolines, isoquinolines and the diazine N-oxides, possessing a variety of substitution patterns. Furthermore, all of the reagents associated are cheap and easy to obtain. The potential extension of this method to a one-pot oxidation/halogenation sequence that obviates the need for isolation of the N-oxide intermediates is also presented.
- Wang, Dong,Wang, Yuxi,Zhao, Junjie,Li, Linna,Miao, Longfei,Wang, Dong,Sun, Hua,Yu, Peng
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p. 5762 - 5768
(2016/08/30)
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- Development of a facile and inexpensive route for the preparation of α-halobenzopyridines from α-unsubstituted benzopyridines
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A facile and inexpensive route for the preparation of α-halobenzopyridines from α-unsubstituted benzopyridines via N-methylbenzopyridin-α-ones was developed. α-Unsubstituted benzopyridines were converted easily into the corresponding N-methylbenzopyridin-α-ones, which were halogenated using PPh3-TCICA or PPh3-DBICA without using solvent to give α-halobenzopyridines.
- Sugimoto, Osamu,Iwasaki, Hyuma,Tanji, Ken-Ichi
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p. 1445 - 1454
(2015/07/15)
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