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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.

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.

journal_name

Bioorg Med Chem

journal_title

Bioorganic & medicinal chemistry

authors

Estévez-Sarmiento F,Said M,Brouard I,León F,García C,Quintana J,Estévez F

doi

10.1016/j.bmc.2017.09.043

subject

Has Abstract

pub_date

2017-11-01 00:00:00

pages

6060-6070

issue

21

eissn

0968-0896

issn

1464-3391

pii

S0968-0896(17)31536-5

journal_volume

25

pub_type

杂志文章

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