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首页> 外文期刊>Dalton transactions: An international journal of inorganic chemistry >Mono- and multimeric ferrocene congeners of quinoline-based polyamines as potential antiparasitics
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Mono- and multimeric ferrocene congeners of quinoline-based polyamines as potential antiparasitics

机译:喹啉基多胺的单和多聚二茂铁同类物作为潜在的抗寄生虫药

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摘要

A series of mono- and multimeric polyamine-containing ferrocenyl complexes containing a quinoline motif were prepared. The complexes were characterised by standard techniques. The molecular structure of the monomeric salicylaldimine derivative was elucidated using single crystal X-ray diffraction and was consistent with the proposed structure. The antiplasmodial activity of the compounds were evaluated in vitro against both the NF54 (chloroquine-sensitive) and K1 (chloroquine-resistant) strains of Plasmodium falciparum. The polyamine derivatives exhibit good resistance index values suggesting that these systems are beneficial in overcoming the resistance experienced by chloroquine. Mechanistic studies suggest that haemozoin formation may be the target of these quinoline complexes in the parasite. Some of the complexes exhibit moderate to high cytotoxicity against WHCO1 oesophageal cancer cells in vitro. The monomeric ferrocenyl-amine complexes exhibit potent activity against this particular cell line. The complexes were also screened against the G3 strain of Trichomonas vaginalis and the salicylaldimine complexes demonstrated promising activity at the tested concentration. All of these compounds show no inhibitory effect on several common normal flora bacteria, indicative of their selectivity for eukaryotic pathogens and cancer.
机译:制备了一系列具有喹啉基序的含单和多聚多胺的二茂铁基络合物。用标准技术表征复合物。使用单晶X射线衍射阐明了单体水杨醛亚胺衍生物的分子结构,并且与提出的结构一致。在体外评估了化合物对恶性疟原虫的NF54(对氯喹敏感)和K1(对氯喹抗性)菌株的抗血浆活性。该多胺衍生物表现出良好的电阻指数值,表明这些体系对于克服氯喹所经历的电阻是有益的。机理研究表明,血红蛋白的形成可能是这些寄生虫中喹啉配合物的目标。某些复合物在体外对WHCO1食道癌细胞具有中等至高的细胞毒性。单体二茂铁基-胺络合物对这种特定细胞系表现出有效的活性。还针对阴道毛滴虫的G3株筛选了复合物,并且水杨醛亚胺复合物在测试浓度下显示出有希望的活性。所有这些化合物对几种常见的正常菌群均无抑制作用,表明它们对真核病原体和癌症的选择性。

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