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  • 标题:Differential Contribution of Metal Complexation and Dimerization to the Chemotherapeutic Potential of Bicyclen-ZnII2 Complex against Human Immunodeficiency Virus
  • 本地全文:下载
  • 作者:Yoshio INOUYE ; Tatsuyuki KANAMORI ; Tetsuya YOSHIDA
  • 期刊名称:Biological and Pharmaceutical Bulletin
  • 印刷版ISSN:0918-6158
  • 电子版ISSN:1347-5215
  • 出版年度:1996
  • 卷号:19
  • 期号:3
  • 页码:456-458
  • DOI:10.1248/bpb.19.456
  • 出版社:The Pharmaceutical Society of Japan
  • 摘要:1, 1'-(m-Xylenediyl)-bis (1, 4, 7, 10-tetraazacyclododecane)-ZnII2 complex (m-xylenediyl-bicyclen-ZnII2), a potent inhibitor of human immunodeficiency virus (HIV), was obtained from cyclen by a combination of dimerization and metal complexation. The ratio of median cytotoxic concentration against host cells (CC50) and median effective concentration against HIV cytopathogenicity (EC50), referred to as the selectivity index (SI), was regarded to be a measure of anti-HIV activity. These two chemical modifications contributed to a potent, in vitro anti-HIV activity of m-xylenediyl-bicyclen-ZnII2 by respectively increasing the CC50 and decreasing the EC50 in comparison with those of cyclen.
  • 关键词:anti-HIV activity;macrocyclic polyamine;cyclen;metal complexation;dimerization
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