<p>New hybrid compounds were synthesized by the reaction of effective inhibitors of human topoisomerase I, natural (5<i>Z</i>,9<i>Z</i>)-eicosa-5,9-dienoic acid and synthetic (5<i>Z</i>,9<i>Z</i>)-phenylundeca-5,9-dienoic acid, with polycyclic amines. The obtained hybrid compounds were found to have pronounced cytotoxic activity against five studied cell lines (Jurkat, U937, K562, HEK293, fibroblasts), with the lead compound showing selective activity against Jurkat and K562 cells; its activity was found to be comparable with that of comparison drugs, camptothecin and etoposide.</p>

错误:搜索内容不能为空,请输入英文关键词
错误:关键词超出字数限制,请精简
高级检索

Synthesis of hybrid compounds based on 5Z,9Z-dienoic acids and polycyclic amines and study of their cytotoxic activity

  • A. A. Makarov,
  • L. U. Dzhemileva,
  • E. Kh. Makarova,
  • U. M. Dzhemilev,
  • V. A. D’yakonov

摘要

New hybrid compounds were synthesized by the reaction of effective inhibitors of human topoisomerase I, natural (5Z,9Z)-eicosa-5,9-dienoic acid and synthetic (5Z,9Z)-phenylundeca-5,9-dienoic acid, with polycyclic amines. The obtained hybrid compounds were found to have pronounced cytotoxic activity against five studied cell lines (Jurkat, U937, K562, HEK293, fibroblasts), with the lead compound showing selective activity against Jurkat and K562 cells; its activity was found to be comparable with that of comparison drugs, camptothecin and etoposide.