ZFIN ID: ZDB-PUB-140528-1
Synthesis, structure-activity relationships and biological evaluation of barbigerone analogues as anti-proliferative and anti-angiogenesis agents
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.
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:
  • Angiogenesis Inhibitors/chemical synthesis
  • Angiogenesis Inhibitors/chemistry*
  • Angiogenesis Inhibitors/pharmacology*
  • Animals
  • Antineoplastic Agents/chemical synthesis*
  • Antineoplastic Agents/chemistry
  • Antineoplastic Agents/pharmacology*
  • Cell Line, Tumor
  • Cell Proliferation/drug effects
  • Dose-Response Relationship, Drug
  • Drug Screening Assays, Antitumor
  • HCT116 Cells
  • Hep G2 Cells
  • Humans
  • Isoflavones/chemical synthesis
  • Isoflavones/chemistry
  • Isoflavones/pharmacology*
  • Molecular Conformation
  • Neovascularization, Physiologic/drug effects*
  • Structure-Activity Relationship
  • Zebrafish
PubMed: 24863745 Full text @ Bioorg. Med. Chem. Lett.
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.