PUBLICATION

Synthesis, structure-activity relationships and biological evaluation of barbigerone analogues as anti-proliferative and anti-angiogenesis agents

Authors
Wang, G., Wang, F., Cao, D., Liu, Y., Zhang, R., Ye, H., Li, X., He, L., Yang, Z., Ma, L., Peng, A., Xiang, M., Wei, Y., Chen, L.
ID
ZDB-PUB-140528-1
Date
2014
Source
Bioorganic & medicinal chemistry letters   24(14): 3158-63 (Journal)
Registered Authors
Wang, Fang
Keywords
Anti-angiogenesis, Anti-proliferative, Barbigerone, Isoflavone
MeSH Terms
  • Structure-Activity Relationship
  • Hep G2 Cells
  • Antineoplastic Agents/chemical synthesis*
  • Antineoplastic Agents/chemistry
  • Antineoplastic Agents/pharmacology*
  • Zebrafish
  • Isoflavones/chemical synthesis
  • Isoflavones/chemistry
  • Isoflavones/pharmacology*
  • Molecular Conformation
  • Animals
  • Neovascularization, Physiologic/drug effects*
  • HCT116 Cells
  • Cell Line, Tumor
  • Cell Proliferation/drug effects
  • Humans
  • Dose-Response Relationship, Drug
  • Drug Screening Assays, Antitumor
  • Angiogenesis Inhibitors/chemical synthesis
  • Angiogenesis Inhibitors/chemistry*
  • Angiogenesis Inhibitors/pharmacology*
PubMed
24863745 Full text @ Bioorg. Med. Chem. Lett.
Abstract
A series of barbigerone analogues (7a-7w, 13a-13x) were designed, synthesized and biologically evaluated for their anti-proliferative and anti-angiogenic activities. Among these compounds, compound 13a exhibited the most potent inhibitory effect on the proliferation of HUVECs, HepG2, A375, U251, B16, and HCT116 cells (IC50=3.80, 0.28, 1.58, 3.50, 1.09 and 0.68 μM, respectively). Compound 13a inhibited the angiogenesis in zebrafish embryo assay in a concentration-dependent manner. Furthermore, 13a also effectively inhibited the migration and capillary like tube formation of human umbilical vein endothelial cell in vitro. These results support the further investigation of this class of compounds as potential anti-proliferative and anti-angiogenesis agents.
Genes / Markers
Figures
Expression
Phenotype
Mutations / Transgenics
Human Disease / Model
Sequence Targeting Reagents
Fish
Antibodies
Orthology
Engineered Foreign Genes
Mapping