Synthesis, characterization and <i>in vitro</i> antitumor behavior of a vanadium(V) complex with 4′-(3-methoxyphenyl)-2,2′:6′2″-terpyridine

<p>A dioxovanadium(V) complex, [VO<sub>2</sub>(moptpy)](ClO<sub>4</sub>) (<b>1</b>, moptpy = 4′-(3-methoxyphenyl)2,2′:6′2″-terpyridine), was synthesized and characterized by elemental analysis, ESI-MS, UV–vis, IR, and <sup>1</sup>H, <sup>13</sup>C, and <sup>51</sup>V NMR. The cytotoxicity <i>in vitro</i> of <b>1</b> was evaluated against cancer cell lines HepG-2 (hepatocellular carcinoma), SGC-7901 (gastric carcinoma), SiHa (cervical cancer), BEL-7402 (hepatocellular), and rat PC-12 (pheochromocytoma) by the MTT method. The results demonstrated that <b>1</b> exhibits superior anticancer activity <i>in vitro</i> with much lower values of 50% inhibitive concentration (IC<sub>50</sub>) against the selected cell lines than cisplatin, and <b>1</b> shows the highest cytotoxic activity toward SGC-7901 cells (IC<sub>50</sub> = 1.3 ± 0.1 μM) among the selected cell lines. A series of cellular morphological and staining experiments were carried out, and the results indicated that <b>1</b> can effectively induce apoptosis of SGC-7901 cells through a ROS-mediated mitochondrial dysfunction pathway. In addition, cellular incorporation and cell cycle analysis were also performed, and it was concluded from the experimental observations that <b>1</b> can efficiently enter into the cell nuclei, and the complex inhibits cell growth in SGC-7901 cell at G0/G1 phase.</p>