Evaluation of the Antiangiogenic Effects of 2-Aryl-3-bromoquinolin-4(1H)-ones and a NCH3-4-oxo Derivative

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概要

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• 2-Aryl-3-bromoquinolin-4(1H)-ones and 2-aryl-3-bromo-1-methylquinolin-4(1H)-one were evaluated for their antiangiogenic effects. Results showed that the 2-aryl-3-bromoquinolin-4(1H)-ones (QNHFBr and QNHClBr), and the 3-bromo-2-(4-chlorophenyl)-1-methylquinolin-4(1H)-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.

• 公益社団法人　日本薬学会の論文

著者

• Mabeta Peace

  Department of Anatomy and Physiology, Private Bag X04, University of Pretoria

• Auer Roland

  University of Pretoria Biomedical Research Centre, University of Pretoria

• Mphahlele Malose

  Department of Chemistry, College of Science, Engineering and Technology, University of South Africa

関連論文

• Evaluation of the Antiangiogenic Effects of 2-Aryl-3-bromoquinolin-4(1H)-ones and a NCH3-4-oxo Derivative

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