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Synthesis and biological evaluation of scopoletin derivatives.

Abstract：

:A series of new scopoletin derivatives were designed and synthesized. Their anti-proliferative effect was initially evaluated against various human cancer cell lines. Among the tested compounds, A1, A2, and D6 showed significant anti-proliferative activities. Angiogenesis was detected by endothelial cell migration assay and tube formation study. The results showed that A1, A2, and D6 inhibited the vascular endothelial growth factor (VEGF)-stimulated proliferation, migration, and tube formation of human umbilical vein endothelial cells in vitro. Moreover, they inhibited the vessel growth in the chorioallantoic membrane in vivo. This inhibition was correlated with a significant decrease in the VEGF-triggered phosphorylated forms of ERK1/2 and Akt. In summary, these findings strongly suggested that these scopoletin derivatives might be structurally novel angiogenesis inhibitors.

journal_name

Bioorg Med Chem

journal_title

Bioorganic & medicinal chemistry

authors

Cai X,Yang J,Zhou J,Lu W,Hu C,Gu Z,Huo J,Wang X,Cao P

doi

10.1016/j.bmc.2012.10.059

subject

Has Abstract

pub_date

2013-01-01 00:00:00

pages

84-92

issue

1

eissn

0968-0896

issn

1464-3391

pii

S0968-0896(12)00889-9

journal_volume

21

pub_type

杂志文章

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