Citation: Xun-Yi LI, Yu-Jing WANG, Zi-Mo ZHOU, Xiao FANG, Qing-Qing WANG, Mei-Chun HU, Xiao-Song YANG, Xiao-Bo WANG. Synthesis, crystal structure, and anticancer activity of a polypyridyl binuclear monofunctional platinum(Ⅱ) complex[J]. Chinese Journal of Inorganic Chemistry, ;2023, 39(1): 141-149. doi: 10.11862/CJIC.2022.272 shu

Synthesis, crystal structure, and anticancer activity of a polypyridyl binuclear monofunctional platinum(Ⅱ) complex

Figures(6)

  • A binuclear monofunctional platinum(Ⅱ) complex, [Pt2(BPA-TPA)Cl2]Cl2 (Pt2-BPA-TPA), containing polypyridyl ligand 2, 6-bis((bis(pyridin-2-ylmethyl)amino)methyl)pyridine was synthesized and characterized by nuclear magnetic resonance and high-resolution mass spectroscopy. In addition, the structure of Pt2-BPA-TPA was determined by X-ray single-crystal diffraction. Agarose gel electrophoresis experiments were used to demonstrate the efficient pBR322 DNA-cleaving activity of Pt2-BPA-TPA at a low concentration of 10 μmol·L-1. In CCK-8 (cell counting kit-8) cytotoxicity studies using the A549 human lung cancer cell line, Pt2-BPA-TPA demonstrated enhanced anticancer activity compared with cisplatin. Mechanistic studies provided evidence that Pt2-BPA-TPA induces apoptosis via triggering DNA damage and upregulating downstream cellular signaling cascades of p21 and cleaved-caspase-3.
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