期刊
BIOORGANIC & MEDICINAL CHEMISTRY
卷 21, 期 1, 页码 84-92出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2012.10.059
关键词
Scopoletin derivative; Angiogenesis; Invasion; Metastasis
资金
- National Natural Science Foundation of China [81274150, 81202967, 30873410]
- Jiangsu Province's Outstanding Leader Program of Traditional Chinese Medicine
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. (C) 2012 Elsevier Ltd. All rights reserved.
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