Abstract

Half-sandwich Cp*-Rh complexes containing curcuminoids ([Rh(η5-Cp*)(L)(Py)]PF6, 1-3, L = curcuminoid ligands L1-L3) were prepared, characterized and studied for anticancer activity. Complex 1 was structurally characterized by single-crystal X-ray crystallography. Complex 3 presented excellent photodynamic anticancer effect in light (>400 nm) showing IC50 values of 7.5 and 4.3 μM against HepG2, SKOV3 and HeLa, respectively, along with the 12.4, 7.9 and 4.7-fold lower toxicity in the dark. Confocal fluorescence images show that the complex primarily targeted mitochondrial localization. These results suggest that the complex 3 was a valuable agent with higher efficacy for chemotherapy and photodynamic therapy, which can achieve real-time image guidance in cancer therapy for the fluorescence of the complex as imaging signals. This investigation provides a valuable route to design novel half-sandwich Cp*-Rh complexes with higher efficacy for photodynamic anticancer chemotherapy.

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