Cancer, a malignant disease, poses a serious threat to global health due to its characteristics of uncontrolled proliferation, transformation, and metastasis. This results in high recurrence and mortality rates, making cancer a challenging medical issue worldwide [1]. In the cancer chemotherapy, a series of platinum metal drugs have been a cornerstone. Their mechanism involves binding to DNA through the aquation of PtCl bonds, resulting in intracellular reduction of chloride ion concentration to approximately 20 mM [2]. However, due to the serious side-effects of cisplatin, a lot of alternative metal-based compounds have been developed. This has brought about the exploration of non‑platinum metal anticancer drugs possessing distinct mechanisms of action. Notably, iridium (III) compounds have shown potential as effective anti-cancer agents, targeting various cellular components such as mitochondria, proteins, DNA, and lysosomes [3,4]. Recent studies have highlighted the numerous iridium (III) complexes demonstrating a prominent efficiency in restraining tumor cell growth [[5], [6], [7], [8], [9], [10], [11], [12], [13], [14], [15]]. on the other hand, photodynamic therapy (PDT) has been considered as another effective method to cure cancer, which uses specific light wavelengths to enhance drug efficacy. Studies by Sun and colleagues have shown that an iridium(III) complex exhibits minimal cytotoxicity (IC50 > 100 μM) to HepG2 cells, however, upon light irradiation (425 nm), the cytotoxicity significantly increases [16]. Similarly, Liu and team found [Ir(piq)2(IPPH)](PF6) exhibiting non-cytotoxic y (IC50 > 100 μM) on A549 cells in the absence of light, whereas its cytotoxicity is markedly enhanced under illumination (IC50 = 0.2 ± 0.05 μM) [17]. Many photosensitizers currently undergoing clinical or pre-clinical studies predominantly affect the mitochondria and induce apoptosis via PDT [18]. Furthermore, liposomes, consisting of phospholipid and cholesterol bilayers, can encapsulate both hydrophilic and lipophilic drugs, significantly enhancing their anticancer efficacy. Our previous studies have demonstrated that liposome-encapsulated iridium(III) complexes exhibit a strong inhibitory effect on cell growth and effectively prevent tumor growth [[19], [20], [21]]. Additionally, we have found iridium (III) complexes with ligands bearing -NH2 group, and their liposome-loaded counterparts, showing significant ability to inhibit cancer cell growth [21,22]. To gain more insights into their anticancer activities, this article introduces pteridino[6,7-f][1,10]phenanthroline-11,13-diamine (PPD), featuring two -NH2 substituent groups as a ligand, two of its iridium (III) complexes (Scheme 1): [Ir(bzq)2(PPD)](PF6) (bzq = deprotonated 2-phenylpyridine) (4a) and [Ir(piq)2(PPD)](PF6) (piq = deprotonated 1-phenylisoquinoline) (4b) were prepared and characterized. Anticancer efficiency of 4a, 4b, and their liposome-loaded forms, 4alip and 4blip, was evaluated under various conditions, including light irradiation.