Ferrocene-modified half-sandwich iridium(III) and ruthenium(II) propionylhydrazone complexes and anticancer application

• Published in: Journal of inorganic biochemistry Vol. 257; p. 112586
• Main Authors: Ji, Changjian, Dong, Ruixiao, Zhang, Pei, Tao, Rui, Wang, Xuan, Dai, Qiaoqiao, Liu, Xicheng, Yuan, Xiang-Ai, Zhang, Shumiao, Yue, Mingbo, Liu, Zhe
• Format: Journal Article
• Language: English
• Published: United States Elsevier Inc 01.08.2024
• Subjects: Anticancer; Ferrocene; Half-sandwich structure; Iridium(III) complex; Ruthenium(II) complex; Ruthenium(II) complex; A549 cells; WCR; MTT; Ferrocene; NAD; DMEM; MTDR; PCC; MMP; Half-sandwich structure; CCCP; TON; Hoechst 33258; NADH; MLCT; LTDR; Iridium(III) complex; ROS; PI; Anticancer; BEAS-2B cells; Fc; JC-1
• ISSN: 0162-0134; 1873-3344; 1873-3344
• DOI: 10.1016/j.jinorgbio.2024.112586

Ferrocene, ruthenium(II) and iridium(III) organometallic complexes, potential substitutes for platinum-based drugs, have shown good application prospects in the field of cancer therapy. Therefore, in this paper, six ferrocene-modified half-sandwich ruthenium(II) and iridium(III) propionylhydrazone complexes were prepared, and the anticancer potential was evaluated and compared with cisplatin. These complexes showed potential in-vitro anti-proliferative activity against A549 cancer cells, especially for Ir-based complexes, and showing favorable synergistic anticancer effect. Meanwhile, these complexes showed little cytotoxicity and effective anti-migration activity. Ir3, the most active complex (ferrocene-appended iridium(III) complex), could accumulate in the intracellular mitochondria, disturb the cell cycle (S-phase), induce the accumulation of reactive oxygen species, and eventually cause the apoptosis of A549 cells. Then, the design of these complexes provides a good structural basis for the multi-active non‑platinum organometallic anticancer complexes. Ferrocene-appended iridium and ruthenium complexes could target mitochondria, disturb cell cycle, induce the increase of reactive oxygen species (ROS) and A549 cell apoptosis. [Display omitted] •Ferrocene-appended half-sandwich iridium and ruthenium complexes were prepared.•Complexes showed favorable anti-proliferative and anti-migration activity.•Complexes could target mitochondria and lead to A549 cell apoptosis.