Multifunctional Heterometallic Ir ^III −Au ^I Probes as Promising Anticancer and Antiangiogenic Agents

A new class of emissive cyclometallated IrIII−AuI complexes with a bis(diphenylphosphino) methanide bridging ligand was successfully synthesised from the diphosphino complex [Ir(N^C)2(dppm)]+ (1). The different gold ancillary ligand, triphenylphosphine (2), chloride (3) or thiocytosine (4) did not reveal any significant effect on photophysical properties, which are mainly due to metal-to-ligand charge-transfer (3MLCT) transitions based IrIII. However, AuI fragment, along seemed crucial for bioactivity in A549 lung carcinoma cells versus endothelial cells. Both cell types display variable sensitivities (IC50=0.6–3.5 μM). apoptotic pathway is activated all cases, and paraptotic death seems take place at initial stages Species 2–4 showed least dual lysosomal mitochondrial biodistribution cells, an localisation possible trafficking process between both organelles time. bimetallic disrupted transmembrane potential increased reactive oxygen species (ROS) generation thioredoxin reductase (TrxR) inhibition comparison that displayed by monometallic 1. Angiogenic activity assays performed revealed promising antimetastatic 1, 2 4.