26021-90-9Relevant articles and documents
Aβ Aggregation inhibitors. Part 1: Synthesis and biological activity of phenylazo benzenesulfonamides
Lin, Shwu-Jiuan,Shiao, Young-Ji,Chi, Chih-Wen,Yang, Li-Ming
, p. 1173 - 1176 (2004)
Phenylazo benzenesulfonamides were designed and synthesized as β-amyloid (Aβ40) fibril assembly inhibitors, and evaluated for inhibition of Aβ40 aggregation and neurotoxicity using rat cortical neurons. Compound 2 (LB-152) was the most potent compound in this study, and the para-NMe2 group on the end of the phenylazo moiety may play an important role in preventing Aβ40 fibril formation. LB-152 provides a new lead for further development of potential β-amyloid aggregation inhibitors to treat AD.
Carbonic anhydrase inhibitors. Diazenylbenzenesulfonamides are potent and selective inhibitors of the tumor-associated isozymes IX and XII over the cytosolic isoforms I and II
Carta, Fabrizio,Maresca, Alfonso,Scozzafava, Andrea,Vullo, Daniela,Supuran, Claudiu T.
experimental part, p. 7093 - 7099 (2010/03/03)
A series of diazenylbenzenesulfonamides, azo-dye derivatives of sulfanilamide or metanilamide incorporating phenol and amine moieties, were tested for inhibition of the tumor-associated isozymes of carbonic anhydrase (CA, EC 4.2.1.1), CA IX and XII. These compounds showed moderate-low inhibitory activities against the cytosolic isoforms CA I and II (offtargets) and excellent, low nanomolar inhibitory activity against the transmembrane CA IX and XII (KIs in the range of 3.5-63 nM against CA IX and 5.0-69.4 nM against CA XII, respectively). The selectivity ratio for inhibiting the tumor-associated CA IX over the offtarget CA II was in the range of 15-104 for these diazenylbenzenesulfonamides, making them among the most isoform-selective inhibitors targeting tumor-associated CAs (over the ubiquitous CA II). Since CA IX/XII were recently shown to be both therapeutic and diagnostic targets for hypoxic solid tumors overexpressing these proteins, such compounds held promise for the management of hypoxic tumors, which are largely non-responsible to classical chemo- and radio-therapy.
STUDY OF THE HYDROLYTIC STABILITY OF 1-ANILINO-1-ALKANESULFONATES BY MEANS OF SPECTRODENSITOMETRIC THIN-LAYER CHROMATOGRAPHY
Nesterenko, S. A.,Bogatchuk, Yu. Ya.,Kofanov, V. I.
, p. 1666 - 1670 (2007/10/02)
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