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摘要
Fifteen organometallic Ir(III) half-sandwich complexes (1A-5C) having the general formula [(eta(5)-Cp-x)Ir(N boolean AND N)Cl]PF6 (Cp-x = Cp*, tetramethyl(phenyl)cyclopentadienyl (Cp-xph) or tetramethyl(biphenyl)cyclopentadienyl (Cp-xbiph); N boolean AND N = diamine) have been synthesized and characterized. The molecular structure of 1A was determined using single-crystal X-ray diffraction analysis. The hydrolysis of 1A-5C was monitored using UV-visible spectra. Complexes 3A-3C showed catalytic activity for the oxidation of NADH to NAD(+), where 3C showed the highest turnover number of 29.9 within 450 min. Cytotoxicity examination by MTT assay was carried out against two human cancer cell lines (HeLa and A549) after 24 or 48 h drug treatment. The complexes showed high potency, where the most potent complex (3C; IC50 = 3.4 mu M) was six times more active than cisplatin against A549 cells after 24 h drug exposure. Cytotoxic potency towards A549 cells increased with phenyl substitution on Cp ring: Cp-xbiph > Cp-xph > Cp*. In addition, the biological studies showed that 3C caused cell apoptosis and cell cycle arrest at G(1) phase in A549 cancer cells. Moreover, 3C increased the level of reactive oxygen species markedly after 24 h, which may provide an important basis for killing cancer cells. Confocal laser scanning microscopy was used to track 3C in A549 cells. The cellular localization experiment showed that 3C targeted lysosomes and caused lysosomal damage.
- 出版日期2019-1
- 单位曲阜师范大学
