40274-67-7Relevant articles and documents
Inhibitory activities of anthraquinone and xanthone derivatives against transthyretin amyloidogenesis
Kitakami, Ryota,Inui, Kishin,Nakagawa, Yusuke,Sawai, Yurika,Katayama, Wakana,Yokoyama, Takeshi,Okada, Takuya,Kanamitsu, Kayoko,Nakagawa, Shinsaku,Toyooka, Naoki,Mizuguchi, Mineyuki
, (2021/07/06)
Transthyretin is a tetrameric protein which functions as a transporter of thyroxine and retinol-binding protein. Misfolding and amyloid aggregation of transthyretin are known to cause wild-type and hereditary transthyretin amyloidosis. Stabilization of the transthyretin tetramer by low molecular weight compounds is an efficacious strategy to inhibit the aggregation pathway in the amyloidosis. Here, we investigated the inhibitory activities of anthraquinone and xanthone derivatives against amyloid aggregation, and found that xanthone-2-carboxylic acid with one chlorine or methyl group has strong inhibitory activity comparable with that of diflunisal, which is one of the best known stabilizers of transthyretin. X-ray crystallographic structures of transthyretin in complex with the compounds revealed that the introduction of chlorine, which is buried in a hydrophobic region, is important for the strong inhibitory effect of the stabilizer against amyloidogenesis. An in vitro absorption, distribution, metabolism and elimination (ADME) study and in vivo pharmacokinetic study demonstrated that the compounds have drug-like features, suggesting that they have potential as therapeutic agents to stabilize transthyretin.
Highly efficient and regiospecific photocyclization of 2,2′-diacyl bixanthenylidenes
Mao, Mao,Wu, Qing-Qing,Ren, Ming-Guang,Song, Qin-Hua
, p. 3165 - 3169 (2011/05/12)
In contrast to the reversible photochemistry of the 2,2′-substituted bixanthenylidenes (1a-f), the photocyclization of 2,2′-diacyl bixanthenylidenes (1g-j) reveals an irreversible process where the initial cyclic intermediate C(E) can undergo a rapid [1,1
Substituted xanthones as antimycobacterial agents*, part 1: Synthesis and assignment of 1H/13C NMR chemical shifts
Pickert, Martina,Frahm, August Wilhelm
, p. 177 - 192 (2007/10/03)
A series of substituted xanthones was synthesized in order to prove the hypothesis that electron-withdrawing substituents enhance the antimycobacterial activity of these compounds, which is described by means of a QSAR equation with 13C NMR che