364-24-9Relevant academic research and scientific papers
Flavone derivatives, preparation method thereof and anticancer agent
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Paragraph 0169-0173, (2018/05/15)
The present invention relates to a flavone derivative, a manufacturing method thereof and an anticancer agent including the same. Compounds represented by chemical formula 1 and chemical formula 2 according to the present invention are excellent in antica
Design, synthesis and biological activity of flavonoid derivatives as selective agonists for neuromedin U 2 receptor
Ma, Ming-Liang,Li, Ming,Gou, Jiao-Jiao,Ruan, Tian-Yu,Jin, Hai-Shan,Zhang, Ling-Hong,Wu, Liang-Chun,Li, Xiao-Yan,Hu, Ying-He,Wen, Ke,Zhao, Zheng
, p. 6117 - 6123 (2015/02/02)
Central neuromedin U 2 receptor (NMU2R) plays important roles in the regulation of food intake and body weight. Identification of NMU2R agonists may lead to the development of pharmaceutical agents to treat obesity. Based on the structure of rutin, a typi
Structure-Activity relationships of targeted RuII(η 6- P -Cymene) anticancer complexes with flavonol-Derived ligands
Kurzwernhart, Andrea,Kandioller, Wolfgang,B?chler, Simone,Bartel, Caroline,Martic, Sanela,Buczkowska, Magdalena,Mühlgassner, Gerhard,Jakupec, Michael A.,Kraatz, Heinz-Bernhard,Bednarski, Patrick J.,Arion, Vladimir B.,Marko, Doris,Keppler, Bernhard K.,Hartinger, Christian G.
, p. 10512 - 10522 (2013/02/22)
RuII(arene) complexes have been shown to be promising anticancer agents, capable of overcoming major drawbacks of currently used chemotherapeutics. We have synthesized RuII(η6-arene) compounds carrying bioactive flavonol ligands with the aim to obtain multitargeted anticancer agents. To validate this concept, studies on the mode of action of the complexes were conducted which indicated that they form covalent bonds to DNA, have only minor impact on the cell cycle, but inhibit CDK2 and topoisomerase IIα in vitro. The cytotoxic activity was determined in human cancer cell lines, resulting in very low IC50 values as compared to other RuII(arene) complexes and showing a structure-activity relationship dependent on the substitution pattern of the flavonol ligand. Furthermore, the inhibition of cell growth correlates well with the topoisomerase inhibitory activity. Compared to the flavonol ligands, the RuII(η6-p-cymene) complexes are more potent antiproliferative agents, which can be explained by potential multitargeted properties.
