A new class of cyclometalated iridium(III) with NCN pincer and meso-phenylcyanamide BODIPY ligands of the formula [Ir(L)(PPY)(Pcyd-BODIPY)], 1, [Ir(L)(PIQ)(Pcyd-BODIPY)], 2, in which HL: 5-methoxy-1,3-bis (1-methyl-1H-benzo[d]imidazol-2-yl)benzene, Pcyd-BODIPY: 8-(4-phenylcyanamide) BODIPY, PPY: 2-phenylpyridine, PIQ: 1-phenylisoquinoline have been synthesized and studied for photodynamic therapy (PDT). The photophysical properties, DNA binding, DNA photocleavage, cellular uptake, thioredoxin reductase activity, reactive oxygen species (ROS) generation, and cellular apoptosis of the complexes have also been studied. Therefore, we present a conceivable biologically applicable PDT modality that develops persuasively designed photoactivatable Ir(III) complexes.