29219-03-2Relevant articles and documents
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
Synthesis and effects on cell viability of flavonols and 3-methyl ether derivatives on human leukemia cells
Burmistrova, Olga,Marrero, María Teresa,Estévez, Sara,Welsch, Isabel,Brouard, Ignacio,Quintana, José,Estévez, Francisco
, p. 30 - 41 (2014/07/22)
Flavonoids are polyphenolic compounds which display an array of biological activities and are considered potential antitumor agents. Here we evaluated the antiproliferative activity of selected synthetic flavonoids against human leukemia cell lines. We found that 4′-bromoflavonol (flavonol 3) was the most potent. This compound inhibited proliferation in a concentration-dependent manner, induced apoptosis and blocked cell cycle progression at the S phase. Cell death was found to be associated with the cleavage and activation of multiple caspases, the activation of the mitogen-activated protein kinase pathway and the up-regulation of two death receptors (death receptor 4 and death receptor 5) for tumor necrosis factor-related apoptosis-inducing ligand. Moreover, combined treatments using 4′-bromoflavonol and TRAIL led to an increased cytotoxicity compared to single treatments. These results provide a basis for further exploring the potential applications of this combination for the treatment of cancer.
Development of flavonoid-based inverse agonists of the key signaling receptor US28 of human cytomegalovirus
Kralj, Ana,Nguyen, Mai-Thao,Tschammer, Nuska,Ocampo, Nicolette,Gesiotto, Quinto,Heinrich, Markus R.,Phanstiel, Otto
, p. 5019 - 5032 (2013/07/26)
A series of 31 chalcone- and flavonoid-based derivatives were synthesized in good overall yields and screened for their inverse agonist activity on the US28 receptor of human cytomegalovirus (HCMV). With one exception (e.g., 2-(5-bromo-2-methoxyphenyl)-3-hydroxy-4H-chromen-4-one), halogen-substituted flavonoids were typically more potent inverse agonists than their related hydro derivatives. While toxicity could be used to partially explain the inverse agonist activity of some members of the series, 5-(benzyloxy)-2-(5-bromo-2- methoxyphenyl)-4H-chromen-4-one (11b) acted on the US28 receptor as a nontoxic, inverse agonist. The full inverse agonism (efficacy, -89%) and potency (EC 50 = 3.5 μM) observed with flavonoid 11b is especially important as it provides both a new tool to study US28 signaling and a potential platform for the future development of HCMV-targeting drugs.