The discovery of half-sandwich iridium complexes containing lidocaine and (pyren-1-yl)ethynyl derivatives of phenylcyanamide ligands for photodynamic therapy.

The successful design, synthesis, characterization, photophysical properties and anticancer mechanistic studies of a series of half-sandwich cyclopentadienyl iridium(iii) complexes of the type [Cp*IrIII (LC)(L1)](PF6 ), 1, and [Cp*IrIII (LC)(L2)](PF6 ), 2, in which Cp* = pentamethylcyclopentadienyl, L1 = 4-(pyren-10-yl)ethynyl-phenylcyanamide, L2 = 4'-(pyren-10-yl)ethynyl-4-cyanamidobiphenyl, and LC = lidocaine, are reported for their application as photodynamic therapy (PDT) agents. The DNA binding, DNA photocleavage, cellular uptake, and apoptosis of the complexes have also been studied.