Organometallic conjugates of artesunate: synthesis and evaluation of anticancer potential

IF 2.1 3区化学 Q3 CHEMISTRY, INORGANIC & NUCLEAR

Journal of Organometallic Chemistry Pub Date : 2025-08-07 DOI:10.1016/j.jorganchem.2025.123804

Leandre van der Merwe, Catherine H. Kaschula, Prinessa Chellan

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Abstract

New organometallic Ru(II), Rh(III) and Ir(III) complexes containing artesunate were synthesised to ascertain the anticancer effect of combining artesunate with different platinum group metal centres. The synthetic approach involved the preparation of two ligands, di(2-pyridyl) methyl amine (L1) and the dipyridyl-artesunate hybrid (L2), followed by complexation with the metal dimers to produce six complexes, C1-C6. All complexes were evaluated for their anticancer activity against two breast cancer cell lines, MCF-7 and MDA-MB-231, in which they showed moderate to low activity. The complexes containing the artesunate moiety, C4-C6, showed higher activity. All complexes had low to no cytotoxicity against the normal breast cell line, MCF-12A, showing potential selectivity for cancerous cells over normal cells. A potential mode of action, through reactive oxygen species generation, was evaluated, and all complexes were found to lead to an increase in ROS levels in the MDA-MB-231 cells.

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青蒿琥酯的有机金属缀合物：抗癌潜力的合成与评价

合成了含有青蒿琥酯的新型有机金属Ru(II), Rh（III）和Ir（III）配合物，以确定青蒿琥酯与不同铂族金属中心结合的抗癌效果。合成方法包括制备两种配体，二（2-吡啶基）甲基胺（L1）和二吡啶基-青蒿琥酯杂化物（L2），然后与金属二聚体络合生成六种配合物C1-C6。所有复合物对两种乳腺癌细胞系MCF-7和MDA-MB-231的抗癌活性进行了评估，其中它们表现出中等至低的活性。含有青蒿素部分的配合物C4-C6表现出较高的活性。所有复合物对正常乳腺细胞系MCF-12A的细胞毒性都很低甚至没有，显示出对癌细胞比正常细胞有潜在的选择性。通过活性氧的产生，评估了一种潜在的作用模式，发现所有复合物都导致MDA-MB-231细胞中ROS水平的增加。

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来源期刊

Journal of Organometallic Chemistry 化学-无机化学与核化学

CiteScore

4.40

自引率

8.70%

发文量

221

审稿时长

36 days

期刊介绍： The Journal of Organometallic Chemistry targets original papers dealing with theoretical aspects, structural chemistry, synthesis, physical and chemical properties (including reaction mechanisms), and practical applications of organometallic compounds. Organometallic compounds are defined as compounds that contain metal - carbon bonds. The term metal includes all alkali and alkaline earth metals, all transition metals and the lanthanides and actinides in the Periodic Table. Metalloids including the elements in Group 13 and the heavier members of the Groups 14 - 16 are also included. The term chemistry includes syntheses, characterizations and reaction chemistry of all such compounds. Research reports based on use of organometallic complexes in bioorganometallic chemistry, medicine, material sciences, homogeneous catalysis and energy conversion are also welcome. The scope of the journal has been enlarged to encompass important research on organometallic complexes in bioorganometallic chemistry and material sciences, and of heavier main group elements in organometallic chemistry. The journal also publishes review articles, short communications and notes.