Half-sandwiched structure iridium­(III) complexes appear to be an attractive organometallic antitumor agents in recent years. Here, four triphenylamine-modified fluorescent half-sandwich iridium­(III) thiosemicarbazone (TSC) antitumor complexes were developed. Because of the “enol” configuration of the TSC ligands, these complexes formed a unique dimeric configuration. Aided by the appropriate fluorescence properties, studies found that complexes could enter tumor cells in an energy-dependent mode, accumulate in lysosomes, and result in the damage of lysosome integrity. Complexes could block the cell cycle, improve the levels of intrastitial reactive oxygen species, and lead to apoptosis, which followed an antitumor mechanism of oxidation. Compared with cisplatin, the antitumor potential in vivo and vitro confirmed that Ir4 could effectively inhibit tumor growth. Meanwhile, Ir4 could avoid detectable side effects in the experiments of safety evaluation. Above all, half-sandwich iridium­(III) TSC complexes are expected to be an encouraging candidate for the treatment of malignant tumors.

N-phenylcarbazole/triphenylamine modified Schiff base half-sandwich ruthenium(ii) compounds showed potential anticancer activity against A549 and HeLa cells.

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