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  • 标题:Thymidine Phosphorylase Inhibitors with a Homophthalimide Skeleton
  • 本地全文:下载
  • 作者:Tetsuya KITA ; Hiroyasu TAKAHASHI ; Yuichi HASHIMOTO
  • 期刊名称:Biological and Pharmaceutical Bulletin
  • 印刷版ISSN:0918-6158
  • 电子版ISSN:1347-5215
  • 出版年度:2001
  • 卷号:24
  • 期号:7
  • 页码:860-862
  • DOI:10.1248/bpb.24.860
  • 出版社:The Pharmaceutical Society of Japan
  • 摘要:Several N-phenylhomophthalimide derivatives were prepared and their inhibitory activity on thymidine phosphorylase/platelet-derived endothelial cell growth factor (TP/PD-ECGF) was assessed. Among them, 2-(2,6-diethylphenyl)-7-nitro-1,2,3,4-tetrahydroisoquinoline-1,3-dione (9) was found to be a more potent inhibitor than the classical inhibitor, 5-nitrouracil (1). Lineweaver-Burk plot analysis indicated that 9 shows mixed-type competitive inhibition TP/PD-ECGF, while 1 is a competitive inhibitor.
  • 关键词:homophthalimide;thymidine phosphorylase;inhibitor;platelet-derived endothelial cell growth factor
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