Synthesis and Anticancer Studies of Pt(II) Complex Derived from 4‐Phenylthiosemicarbazone

Although cisplatin is widely used as a first-line chemotherapy agent, it has significant side effects. Herein, we synthesized a Pt(II) complex (Pt1) derived from o-vanillin-4-phenylthiosemicarbazone ligand, and confirmed its crystal structure by X-ray crystallography. Complex Pt1 exhibited potent anticancer activity against various tested cancer cell lines, with particular efficacy against HepG-2 cells. Further investigations revealed that Pt1 inhibited the growth of HepG-2 cells through multiple mechanisms, including the generation of excessive reactive oxygen species (ROS), induction of DNA damage, enhancement of mitochondrial membrane permeability, promotion of apoptosis, and activation of autophagic cell death.