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Updated: Aug 6, 2026

Functionalized Spirocyclic Heterocycle Synthesis and Cytotoxicity Assay
Published on: February 9, 2021
Imidazole-based Ru(III) complexes: synthesis, characterisation and anticancer activity
Manel Estruch-Blasco1, Jose Manuel Calderón-Montaño2, Eleuterio Álvarez3
1Departamento de Química Orgánica y Farmacéutica, Facultad de Farmacia, Universidad de Sevilla, c/Profesor García González, 2, 41012, Sevilla, Spain. mpernia@us.es.
None:
In this work, we prepared a series of substituted imidazole-derived Ru(III) complexes, ImRu1-ImRu5, analogous to the clinically evaluated NAMI-A. These Ru(III) complexes, with different functional groups on the imidazole ring, were characterised by 1H NMR and UV-Vis spectroscopy, elemental analysis, low- and high-resolution mass spectrometry, and single crystal X-ray diffraction. The cytotoxicity of the Ru(III) complexes was evaluated in vitro against different cancer and non-cancer cell lines, exhibiting low cytotoxicity activity and antimigratory characteristics comparable to those of the NAMI-A complex, except for the Ru(III) complex bearing an alkyne substituent on the imidazole ring (ImRu3). ImRu3 exhibited selective cytotoxicity against A549, MeWo and T24 cells, while retaining antimigratory activity against T24 cells, indicating that modifications at the imidazole ligand can modulate biological behaviour. Computational and fluorescence studies suggest that functional variations of the imidazole ligand enhance albumin-binding affinity, potentially facilitating transport and contributing to the observed anticancer activity.
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