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Synthesis, Characterization and Anticancer Activities of Metal Complexes

A Special Issue of Molecules (ISSN 1420-3049) belonging to the section "Inorganic Chemistry".

Deadline for manuscript submissions: closed (30 June 2026) | Viewed by 1718

Editor


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Guest Editor
Department of Human Biology, Faculty of Health Sciences, University of Cape Town, Anzio Road, Observatory 7925, Cape Town, South Africa
Interests: bioinorganic chemistry; metal-based anticancer drugs; catalysis; main group organometallic chemistry
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Special Issue Information

Dear Colleagues,

I am excited to serve as the editor for this Special Issue devoted to the Synthesis, Characterisation and Anticancer Activities of Metal Complexes. In recent years, this field has witnessed remarkable progress. Many rationally designed metal complexes have demonstrated excellent anticancer profiles across a variety of cancer cell lines. In-depth biological studies have shed light on diverse cell death mechanisms and emphasized the essential role of the metal center in these processes.

One particularly promising area of advancement is the development of multimetallic complexes, which incorporate two or more metal atoms in well-defined structures, often bridged by coordinating ligands. These complexes offer the potential for synergistic effects and enhanced selectivity, with designs tailored to specifically target cancer cells while sparing healthy ones.
A future direction with significant promise is the translation of in vitro findings into in vivo studies using animal models—an important step toward preclinical development.

We warmly invite submissions of original research articles and reviews that fall within the scope of this exciting and evolving field. We look forward to your contributions and to highlighting the latest developments in this area.

Dr. Burgert Blom
Guest Editor

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Keywords

  • in vitro activity
  • in vivo activity
  • metal complex
  • biological studies
  • anticancer activity
  • bimetallic complexes
  • mechanistic studies

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Published Papers (2 papers)

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Research

18 pages, 13492 KB  
Article
Effect of the µ-Diphosphine Bridging Ligand on the Cytotoxic Activity of Homodinuclear Ruthenium Complexes
by Basile Roufosse, Kathia L. Jiménez-Monroy, Christoph Marschner, Jill van de Laarschot, Oscar Loftus, Thomas J. Cleij, Sharon Prince and Burgert Blom
Molecules 2026, 31(17), 2968; https://doi.org/10.3390/molecules31172968 - 25 Aug 2026
Viewed by 657
Abstract
Herein we report the synthesis and full characterisation of Ru(II)-based homobimetallic complexes bridged by diphosphines of the type [{(p-cym)RuCl2}2(µ-dppx)], where p-cym = η6-1-isopropyl-4-methylbenzene, dppx = dppe (1,2-bis(diphenylphosphino)ethane, 1), tdppe (trans-1,2-bis(diphenylphosphino)ethylene, 2 [...] Read more.
Herein we report the synthesis and full characterisation of Ru(II)-based homobimetallic complexes bridged by diphosphines of the type [{(p-cym)RuCl2}2(µ-dppx)], where p-cym = η6-1-isopropyl-4-methylbenzene, dppx = dppe (1,2-bis(diphenylphosphino)ethane, 1), tdppe (trans-1,2-bis(diphenylphosphino)ethylene, 2), dppa (bis(diphenylphosphino)acetylene, 3), dcpe (1,2-bis(dicyclohexylphosphino)ethane, 4), and 1,4dppb (1,4-bis(diphenylphosphino)benzene, 5). We also report the mononuclear complexes [(p-cym)RuCl21-dppx)], where dppx = dppe (6) and tdppe (7). Complexes 2, 4, 5, 6 and 7 were further characterised via single crystal X-ray diffraction analysis. The bimetallic complexes were synthesised in a straightforward fashion and isolated in good to excellent yields. The mononuclear complexes 6 and 7 are stable in air but exhibit reactions in solution, hindering their use as precursors for the synthesis of bimetallic complexes. The in vitro cytotoxic (anticancer) activities of complexes 15 were determined via cell viability studies and their IC50 values were derived on HeLa and Ect1/E6E7 cell lines. All complexes displayed only low to moderate activity and selectivity. Strikingly, the cytotoxic profiles of the different complexes varied substantially, highlighting the importance of the bridging ligand itself in the cytotoxic behaviour of the complexes, further demonstrating the importance of ligand design in bimetallic complexes. Full article
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24 pages, 17615 KB  
Article
Synthesis and Antitumor Mechanism of Emodin-Derived Transition Metal Complexes
by Yumin Pan, Ying Rui, Biqun Zou, Xiaoteng Jing, Ruijie He, Jianyi Liang and Fangyao Li
Molecules 2026, 31(15), 2682; https://doi.org/10.3390/molecules31152682 - 31 Jul 2026
Viewed by 401
Abstract
In this study, emodin was used as the starting material to synthesize two novel ligands, L1 and L2, containing bipyridine or phenanthroline moieties. Seven metal complexes (1–7) were obtained through coordination with Co, Rh, Ru, and Pt ions. Their structures [...] Read more.
In this study, emodin was used as the starting material to synthesize two novel ligands, L1 and L2, containing bipyridine or phenanthroline moieties. Seven metal complexes (1–7) were obtained through coordination with Co, Rh, Ru, and Pt ions. Their structures were confirmed via NMR, HRMS, UV–Vis, IR, HPLC and SC-XRD analyses. The MTT assay showed that L1 and complex 2 selectively inhibited HepG-2 cells, with IC50 values of 8.77 μM and 6.10 μM, respectively. Both compounds exhibited stronger activity than cisplatin (9.05 μM) and low toxicity toward normal 293T cells. Mechanistic studies demonstrated that they induced G2/M phase arrest by regulating Cyclin B1 and P21 expression, which was accompanied by ROS and Ca2+ accumulation, mitochondrial membrane potential disruption, and activation of the Caspase-9/3 cascade. Complex 2 showed superior antitumor activity to L1, and this finding was further supported by molecular docking analysis. In sum, Rh(III) complex 2 was identified as a selective and mechanistically defined anti-hepatocellular carcinoma lead compound, providing a potential strategy for the development of natural product-based metal anticancer agents. Full article
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