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  • 标题:Evaluation of the Antiangiogenic Effects of 2-Aryl-3-bromoquinolin-4(1H)-ones and a NCH3-4-oxo Derivative
  • 本地全文:下载
  • 作者:Peace Mabeta ; Roland Auer ; Malose Jack Mphahlele
  • 期刊名称:Biological and Pharmaceutical Bulletin
  • 印刷版ISSN:0918-6158
  • 电子版ISSN:1347-5215
  • 出版年度:2009
  • 卷号:32
  • 期号:5
  • 页码:937-940
  • DOI:10.1248/bpb.32.937
  • 出版社:The Pharmaceutical Society of Japan
  • 摘要:2-Aryl-3-bromoquinolin-4(1 H )-ones and 2-aryl-3-bromo-1-methylquinolin-4(1 H )-one were evaluated for their antiangiogenic effects. Results showed that the 2-aryl-3-bromoquinolin-4(1 H )-ones (QNHFBr and QNHClBr), and the 3-bromo-2-(4-chlorophenyl)-1-methylquinolin-4(1 H )-one (QNMeClBr) reduced endothelial cell numbers in an assay of cell proliferation, showing increased cytotoxicity at higher doses. The compounds also inhibited neovessel growth in an ex vivo assay of angiogenesis. Furthermore, low levels of proangiogenic factors, namely, basic fibroblast growth factor (bFGF) and vascular endothelial growth factor/placental growth factor (VEGF/PlGF) were obtained in cultures treated with these compounds. Thus, the tested compounds, QNHFBr, QNHClBr, and QNMeClBr exhibit antiangiogenic activity.
  • 关键词:quinolone derivative;angiogenesis;basic fibroblast growth factor;vascular endothelial growth factor;placental growth factor
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