School of Chemistry and Materials Science, Nanjing Normal University, Nanjing 210023, China.
School of Chemistry and Materials Science, Nanjing Normal University, Nanjing 210023, China.
J Inorg Biochem. 2022 Oct;235:111913. doi: 10.1016/j.jinorgbio.2022.111913. Epub 2022 Jul 6.
9-Anthracenecarboxylic acid (9-Ac) was reported early as a chloride channel inhibitor and was found to exhibit significant anti-proliferative activity on leukemic cells, but has not been researched in solid tumor cells. Herein, a 9-anthraceneic acid derivative was introduced into the cyclometalated Iridium (III) species to construct a novel Iridium (Ir) complex Ir-9-Ac, [Ir(ppy)(9-Ac-L)]PF (ppy = 2-phenylpyridine, 9-Ac-L = N-((4'-methyl-[2,2'-bipyridin]-4-yl)methyl)anthracene-9-carboxamide), which could accumulated in lysosomes. Ir-9-Ac showed good cytotoxic activity against several tumor cell lines, notably on A549 cells. Besides Ir-9-Ac could inhibit the cell colony formation and growth of the 3D cell spheroids, demonstrating the potential to suppress tumors in vivo. This design provided a platform for the design of cyclometalated Iridium (III) anticancer complexes.
9-蒽羧酸（9-Ac）早期被报道为氯离子通道抑制剂，并且被发现对白血病细胞具有显著的抗增殖活性，但尚未在实体肿瘤细胞中进行研究。在此，将 9-蒽酸衍生物引入环金属化铱（III）物种中，构建了一种新型铱（Ir）配合物 Ir-9-Ac，[Ir（ppy）（9-Ac-L）]PF（ppy=2-苯基吡啶，9-Ac-L=N-（（4'-甲基-[2,2'-联吡啶]-4-基）甲基）蒽-9-甲酰胺），它可以在溶酶体中积累。Ir-9-Ac 对多种肿瘤细胞系表现出良好的细胞毒性活性，特别是对 A549 细胞。此外，Ir-9-Ac 可以抑制 3D 细胞球状体的细胞集落形成和生长，表明其在体内抑制肿瘤的潜力。该设计为设计环金属化铱（III）抗癌配合物提供了一个平台。
