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.