- PENTAFLUOROPHENYL SULFONAMIDE COMPOUNDS, COMPOSITIONS AND USES THEREOF
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The present application relates to sulfonamide containing compounds of Formulae (I) and (II) and compositions containing said compounds effective in the treatment of cell proliferative disorders, in particular cancer, and various methods of use thereof.
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Paragraph 00134; 00236
(2019/04/16)
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- Carbonic anhydrase inhibitors: Inhibition of the tumor-associated isozyme IX with fluorine-containing sulfonamides. The first subnanomolar CA IX inhibitor discovered
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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.
- Vullo, Daniela,Scozzafava, Andrea,Pastorekova, Silvia,Pastorek, Jaromir,Supuran, Claudiu T.
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p. 2351 - 2356
(2007/10/03)
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- Trimethylsilylesters of Fluorobenzenesulfonic acids
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Fluorobenzenesulfonic acids were prepared by electrophilic sulfonation of fluorobenzenes 1.The acids are obtained as hydrates and converted to their trimethylsilyl esters 2 for characterization.
- Johannsen, Heiner,Sartori, Peter
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p. 674 - 679
(2007/10/02)
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