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Synthesis and anticancer evaluation of mitochondria-targeted half-sandwich Ir(III) and Ru(II) complexes with coumarin-hydrazide ligands
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DOI：10.1016/j.molstruc.2026.146177.png)
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Abstract
En 中文
Coumarin derivatives have received considerable attention because of their diverse biological activities and inherent fluorescence, whereas metal-hydrazide complexes exhibit notable antitumor potential. To merge these complementary features within a single molecular platform, we rationally designed and synthesized a collection of half-sandwich Ir(III) and Ru(II) complexes incorporating coumarin-hydrazide (N<^>O) chelating ligands. The structures of these complexes were comprehensively characterized by multiple analytical techniques, and their photoluminescence behavior together with biological activities was systematically investigated. Notably, the complexes show satisfactory aqueous stability with only gradual hydrolysis and exhibit cytotoxicity comparable to that of cisplatin. Incorporation of the coumarin moiety endows the complexes with pronounced fluorescence, enabling real-time visualization and mechanistic investigation of their anticancer activity. Confocal microscopy revealed that these complexes are internalized predominantly via an energy-coupled pathway and preferentially accumulate in mitochondria. As a result, they induce apoptosis by disrupting mitochondrial membrane potential (MMP) and promoting excessive generation of reactive oxygen species (ROS). In addition, the complexes perturb cell-cycle progression, leading to G0/G1 phase arrest, with the capacity to effectively block cancer cell migration in vitro.
Keywords:
Half sandwich
Iridium
Ruthenium
Coumarin
Acyl hydrazide
Cytotoxicity
Mitochondrial targeting
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4.7
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3.5W
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6.6W
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