title: 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.
authors.affiliation: Laboratory of Cellular and Molecular Biology, Jiangsu Province Academy of Traditional Chinese Medicine, 100# Shizi Street, Hongshan Road, Nanjing 210028, Jiangsu, China.
authors.forename: Xueting
authors.initials: X
authors.lastname: Cai
authors.forename: Jie
authors.initials: J
authors.lastname: Yang
authors.forename: Jinpei
authors.initials: J
authors.lastname: Zhou
authors.forename: Wuguang
authors.initials: W
authors.lastname: Lu
authors.forename: Chunping
authors.initials: C
authors.lastname: Hu
authors.forename: Zhenhua
authors.initials: Z
authors.lastname: Gu
authors.forename: Jiege
authors.initials: J
authors.lastname: Huo
authors.forename: Xiaoning
authors.initials: X
authors.lastname: Wang
authors.forename: Peng
authors.initials: P
authors.lastname: Cao
mesh_terms: D020533:Angiogenesis Inhibitors / Q000737:chemistry* / Q000494:pharmacology*; D000970:Antineoplastic Agents / Q000737:chemistry* / Q000494:pharmacology*; D045744:Cell Line, Tumor; D002465:Cell Movement / Q000187:drug effects; D049109:Cell Proliferation / Q000187:drug effects; D061307:Human Umbilical Vein Endothelial Cells; D006801:Humans; D009369:Neoplasms / Q000188:drug therapy; D012603:Scopoletin / Q000737:chemistry* / Q000494:pharmacology*; D042461:Vascular Endothelial Growth Factor A / Q000378:metabolism
chemical_list: D020533:Angiogenesis Inhibitors; D000970:Antineoplastic Agents; D042461:Vascular Endothelial Growth Factor A; D012603:Scopoletin