Two novel cyclometalated iridium(III) complexes containing fluorinated phenylpyridine (TFPPy)₂IrPic or phenylquinoline (TFPQ)₂IrPic with pyridine-2-carboxylate as chelating ligands were synthesized and fully characterized. These complexes displayed hypoxia sensing and therapeutical activities. As hypoxia probes these two complexes achieved S/B ratio of 7.125; 8.156. Besides the anti-proliferation activities against Cisplatin-resistant cancer cells, radiosensitization effect with SER value 1.742–1.941 were observed even in radio-resistant cell lines after treatment with these complexes, mechanism confirmed via typical G2 phase arrest. Furthermore, the two complexes have shown antiviral activity against both HSV-1 and HSV-2 virus strands. Molecular docking calculation have revealed that this type of Ir(III) complex forms stable hydrogen bond and hydrophobic interactions to the major groove of the double helix of HSV. These findings demonstrated (TFPPy)₂IrPic and (TFPQ)₂IrPic as promising candidates for further evaluation as a novel prodrug platform for combination therapy (RT-CT). © 2020 Elsevier B.V. All rights reserved.

两种新型的含氟化苯基吡啶（TFPPy）₂ IrPic或苯基喹啉（TFPQ）₂ IrPic的环金属化铱（III）配合物以吡啶-2-羧酸盐为螯合配体进行了合成和充分表征。这些复合物表现出缺氧感测和治疗活性。作为缺氧探针，这两种复合物的S / B比为7.125；8.156。除了对顺铂耐药细胞的抗增殖活性外，甚至在用这些复合物处理后的放射抗性细胞系中也观察到了SER值为1.742–1.941的放射增敏作用，其机制通过典型的G2期阻滞得以证实。此外，两种复合物均显示出针对HSV-1和HSV-2病毒链的抗病毒活性。分子对接计算表明，这种类型的Ir（III）配合物与HSV双螺旋的主要凹槽形成稳定的氢键和疏水相互作用。这些发现证明了（TFPPy）₂ IrPic和（TFPQ）₂ IrPic作为有希望的候选者，可以作为一种新型的联合治疗前药平台（RT-CT）进行进一步评估。©2020 Elsevier BV保留所有权利。