5Z、9z二烯酸和多环胺杂化化合物的合成及其细胞毒活性研究

IF 1.7 4区化学 Q3 CHEMISTRY, MULTIDISCIPLINARY

Russian Chemical Bulletin Pub Date : 2025-08-16 DOI:10.1007/s11172-025-4706-3

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

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引用次数: 0

摘要

将人拓扑异构酶I的有效抑制剂天然(5Z,9Z)-二碳二烯酸与合成(5Z,9Z)-苯基十一烷-5,9-二烯酸与多环胺反应合成新的杂化化合物。所获得的杂交化合物对5种所研究的细胞系（Jurkat、U937、K562、HEK293、成纤维细胞）具有明显的细胞毒活性，其中先导化合物对Jurkat和K562细胞具有选择性活性；其活性与比较药物喜树碱和依托泊苷相当。

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

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.

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来源期刊

Russian Chemical Bulletin 化学-化学综合

CiteScore

2.70

自引率

47.10%

发文量

257

审稿时长

3-8 weeks

期刊介绍： Publishing nearly 500 original articles a year, by leading Scientists from Russia and throughout the world, Russian Chemical Bulletin is a prominent international journal. The coverage of the journal spans practically all areas of fundamental chemical research and is presented in five sections: General and Inorganic Chemistry; Physical Chemistry; Organic Chemistry; Organometallic Chemistry; Chemistry of Natural Compounds and Bioorganic Chemistry.