A new class of luminescent Ir^III antitumor agents, namely, [Ir(CP1)(PY1)₂] (Ir-1), [Ir(CP1)(PY2)₂] (Ir-2), [Ir(CP1)(PY4)₂] (Ir-3), [Ir(CP2)(PY1)₂] (Ir-4), [Ir(CP2)(PY4)₂] (Ir-5), [Ir(CP3)(PY1)₂]⋅CH₃OH (Ir-6), [Ir(CP4)(PY4)₂]⋅CH₃OH (Ir-7), [Ir(CP5)(PY2)₂] (Ir-8), [Ir(CP5)(PY4)₂]⋅CH₃OH (Ir-9), [Ir(CP6)(PY1)₂] (Ir-10), [Ir(CP6)(PY2)₂]⋅CH₃OH (Ir-11), [Ir(CP6)(PY3)₂] (Ir-12), [Ir(CP6)(PY41)₂] (Ir-13), and [Ir(CP7)(PY1)₂] (Ir-14), supported by 8-oxychinolin derivatives and 1-phenylpyrazole ligands was prepared. Compared with SK-OV-3/DDP and HL-7702 cells, the Ir-1−Ir-14 compounds exhibited half maximal inhibitory concentration (IC₅₀) values within the high nanomolar range (50 nM−10.99 μM) in HeLa cells. In addition, Ir-1 and Ir-3 accumulated and stained the mitochondrial inner membrane of HeLa cells with high selectivity and exhibited a high antineoplastic activity in the entire cervical HeLa cells, with IC₅₀ values of 1.22 ± 0.36 μM and 0.05 ± 0.04 μM, respectively. This phenomenon induced mitochondrial dysfunction, suggesting that these cyclometalated Ir^III complexes can be potentially used in biomedical imaging and Ir(III)-based anticancer drugs. Furthermore, the high cytotoxicity activity of Ir-3 is correlated with the 1-phenylpyrazole (H-PY4) secondary ligands in the luminescent Ir^III antitumor complex.

一类新的发光Ir ^III抗肿瘤药，即[Ir（CP1）（PY1）₂ ]（Ir-1），[Ir（CP1）（PY2）₂ ]（Ir-2），[Ir（CP1）（ PY4）₂ ]（Ir-3），[Ir（CP2）（PY1）₂ ]（Ir-4），[Ir（CP2）（PY4）₂ ]（Ir-5），[Ir（CP3）（PY1）₂ ]⋅CH ₃ OH（铱6），物[Ir（CP4）（PY4）₂ ]⋅CH ₃ OH（铱7），物[Ir（CP5）（PY2）₂ ]（铱8），的[Ir （CP5）（PY4）₂ ]⋅CH ₃ OH（Ir-9），[Ir（CP6）（PY1）₂ ]（Ir-10），[Ir（CP6）（PY2 ）₂ ]·CH ₃ OH（Ir-11），[Ir（CP6）（PY3）₂ ]（Ir-12），[Ir（CP6）（PY41）₂ ]（Ir-13）和[Ir（CP7）（PY1）₂ ]（Ir-14），由8-氧代喹啉衍生物和1-苯基吡唑支撑制备了配体。与SK-OV-3 / DDP和HL-7702细胞中，比较IR-1 -的Ir-14化合物显示出半数抑制浓度（IC ₅₀）在HeLa细胞中的高纳摩尔范围内（50介于100nM-10.99μM）内的值。此外，Ir-1和Ir-3以高选择性积聚并染色HeLa细胞的线粒体内膜，并在整个宫颈HeLa细胞中表现出高抗肿瘤活性，IC ₅₀值分别为1.22±0.36μM和0.05±0.04μM。这种现象引起线粒体功能障碍，表明这些环金属化的Ir ^III复合物可潜在地用于生物医学成像和基于Ir（III）的抗癌药物。此外，Ir-3的高细胞毒性活性与发光的Ir ^III抗肿瘤复合物中的1-苯基吡唑（H-PY4）二级配体相关。