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3'-Hydroxy-3,4'-dimethoxyflavone Blocks Tubulin Polymerization and Is a Potent Apoptotic Inducer in Human SK-MEL-1 Melanoma Cells

Francisco Estévez-Sarmiento, Mercedes Said, Ignacio Brouard, Francisco León, Celina García, José Quintana, Francisco Estévez

Bioorg Med Chem. 2017 Nov 1;25(21):6060-6070.

PMID: 29032930

Abstract:

Flavonoids 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.

Chemicals Related in the Paper:

Catalog Number Product Name Structure CAS Number Price
AP4143628 3′,4′-Dimethoxyflavone 3′,4′-Dimethoxyflavone 4143-62-8 Price
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