Synthesis, crystal structure and antiproliferative mechanisms of gallium(iii) complexes with benzoylpyridine thiosemicarbazones. Issue 32 (18th May 2020)

• Record Type: Journal Article
• Authors: Qi, Jinxu; Liu, Taichen; Zhao, Wei; Zheng, Xinhua; Wang, Yihong
• Is Part Of: RSC advances. Volume 10:Issue 32(2020)
• Page Start: 18553
• Page End: 18559
• Publication Date: 2020-05-18
• Subjects: Chemistry -- Periodicals; 540.5
• DOI: 10.1039/d0ra02913k
• Languages: English
• ISSNs: 2046-2069

Abstract

Abstract : Ga(iii ) complex promotes apoptosis by consuming intracellular iron, enhancing intracellular reactive oxygen species (ROS), activating caspase-3/9, releasing cytochromes and apoptotic protease activating factor-1 (apaf-1). Abstract : We have prepared six thiosemicarbazone ligands and synthesized the corresponding Ga(iii ) complexes. The antitumor activity of the ligand increases with its lipophilicity, and the antitumor activity of the Ga(iii ) complexes is affected by the ligands. Since C6 has the highest anticancer proliferative activity (0.14 ± 0.01 μM) against HepG-2 (Human hepatocarcinoma cell line), we characterized its structure by X-ray single crystal diffraction and explored its antiproliferation mechanism. Anti-tumor mechanism results show that Ga(iii ) complex (C6 ) promoted HepG-2 cell cycle arrest in the G1 phase by regulating the expression of cell cycle-associated proteins (Cdk 2, cyclin A and cyclin E). Ga(iii ) complex (C6 ) promotes apoptosis by consuming intracellular iron, enhancing intracellular reactive oxygen species (ROS), activating caspase-3/9, releasing cytochromes and apoptotic protease activating factor-1 (apaf-1).