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
-
- 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.
Citation
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. (2014) Synthesis, structure-activity relationships and biological evaluation of barbigerone analogues as anti-proliferative and anti-angiogenesis agents. Bioorganic & medicinal chemistry letters. 24(14):3158-63.
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
Expression
Phenotype
Mutations / Transgenics
Human Disease / Model
Sequence Targeting Reagents
Fish
Orthology
Engineered Foreign Genes
Mapping