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Title: Synthesis and effects on cell viability of flavonols and 3-methyl ether derivatives on human leukemia cells
Authors: Burmistrova, Olga
Marrero, María Teresa
Estévez, Sara 
Welsch, Isabel
Brouard, Ignacio
Quintana, Jose 
Estévez, Francisco 
Keywords: Apoptosis
Death, et al
Issue Date: 2014
Publisher: 0223-5234
Project: Evaluación de Potenciales Compuestos Antileucémicos. 
Journal: European Journal of Medicinal Chemistry 
Abstract: 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. (c) 2014 Elsevier Masson SAS. All rights reserved.
ISSN: 0223-5234
DOI: 10.1016/j.ejmech.2014.07.010
Source: European Journal of Medicinal Chemistry[ISSN 0223-5234],v. 84, p. 30-41
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