107535-73-9Relevant articles and documents
Carbonic anhydrase inhibitors: Inhibition of the tumor-associated isozyme IX with fluorine-containing sulfonamides. The first subnanomolar CA IX inhibitor discovered
Vullo, Daniela,Scozzafava, Andrea,Pastorekova, Silvia,Pastorek, Jaromir,Supuran, Claudiu T.
, p. 2351 - 2356 (2004)
Polyfluorinated CAIs show very good inhibitory properties against different carbonic anhydrase (CA) isozymes, such as CA I, II, and IV, but such compounds have not been tested for their interaction with the transmembrane, tumor-associated isozyme CA IX. Thus, a series of such compounds has been obtained by attaching 2,3,5,6-tetrafluorobenzoyl- and 2,3,5,6- tetrafluorophenylsulfonyl- moieties to aromatic/heterocyclic sulfonamides possessing derivatizable amino moieties. Some of these compounds showed excellent CA IX inhibitory properties and also selectivity ratios favorable to CA IX over CA II, the other physiologically relevant isozyme with high affinity for sulfonamide inhibitors. The first subnanomolar and rather selective CA IX inhibitor has been discovered, as the 2,3,5,6-tetrafluorobenzoyl derivative of metanilamide showed an inhibition constant of 0.8nM against hCA IX, and a selectivity ratio of 26.25 against CA IX over CA II. Several other low nanomolar CA IX inhibitors were detected among the new derivatives reported here. The reported derivatives constitute valuable candidates for the development of novel antitumor therapies based on the selective inhibition of tumor-associated CA isozymes.
Synthesis, structural characterization and antimycobacterial evaluation of several halogenated non-nitro benzothiazinones
Madikizela, Balungile,Eckhardt, Tamira,Goddard, Richard,Richter, Adrian,Lins, Anika,Lehmann, Christoph,Imming, Peter,Seidel, Rüdiger W.
, p. 1523 - 1533 (2021)
8-Nitro-1,3-benzothiazin-4-ones (BTZs), with BTZ043 and PBTZ169 as the most advanced compounds, represent a new class of potent antitubercular agents, which irreversibly inhibit decaprenylphosphoryl-β-d-ribose-2′-epimerase (DprE1), an enzyme crucial for c
Preparation method of tetrafluorobenzene methanol
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Paragraph 0035; 0036, (2019/02/13)
Belonging to the technical field of organic synthesis, the invention discloses a preparation method of tetrafluorobenzene methanol. The method includes: reacting tetrafluorobenzoic acid with thionyl chloride to produce tetrafluorobenzoyl chloride, then taking tetrafluorobenzoyl chloride as the raw material, and conducting reduction in water with sodium borohydride activated by an ether solvent toobtain tetrafluorobenzene methanol. According to the invention, the ether solvent and sodium borohydride are subjected to complexing to activate sodium borohydride, water is adopted as the solvent forreduction, the reaction yield is high, the reductant sodium borohydride can complete the reaction at a catalytic amount, and the reaction process is greener and more environmentally friendly.
