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Title

3′-Hydroxy-3,4′-dimethoxyflavone blocks tubulin polymerization and is a potent apoptotic inducer in human SK-MEL-1 melanoma cells

AuthorsEstévez-Sarmiento, Francisco; Said, Mercedes; Brouard, Ignacio ; León, Francisco ; García, Celina; Quintana, José; Estévez, Francisco
KeywordsMelanoma
Caspases
Cytotoxicity
Flavonoids
Apoptosis
Issue Date1-Nov-2017
PublisherPergamon Press
CitationBioorganic and Medicinal Chemistry 25(21): 6060-6070 (2017)
AbstractFlavonoids are naturally occurring polyphenolic compounds and are among the most promising anticancer agents. A series of flavonols and their 3-methyl ether derivatives were synthesized and assessed for cytotoxicity. It was found that 3′-hydroxy-3,4′-dimethoxyflavone (flavonoid 7a) displayed strong cytotoxicity against human SK-MEL-1 melanoma cells and blocked tubulin polymerization, but had no significant cytotoxic effects against quiescent or proliferating human peripheral blood mononuclear cells. Our analyses showed that flavonoid 7a induces G2-M cell cycle arrest and apoptosis in melanoma cells which is associated with cytochrome c release and activation of both extrinsic and intrinsic apoptotic pathways of cell death.
Publisher version (URL)https://doi.org/10.1016/j.bmc.2017.09.043
URIhttp://hdl.handle.net/10261/185169
DOI10.1016/j.bmc.2017.09.043
ISSN0968-0896
E-ISSN1464-3391
Appears in Collections:(IPNA) Artículos
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