Mixed-ligand Cu(II) hydrazone complexes designed to enhance anticancer activity

European Journal of Medicinal Chemistry
QingYou MoFeng Yang

Abstract

The ligand quantity, ligand type, and coordination geometry have important influences on the anticancer activity of metal-based complexes. On the basis of the structures of previously reported 1:1 Cu(II)/ligand complexes ([Cu(L1)Cl]·2H2O 1a, [Cu(L2)Cl]·H2O 2a, and [Cu(L2)NO3]·H2O 3a), we subsequently designed, developed, and characterized a series of corresponding 1:1:1 Cu(II)/ligand/co-ligand complexes ([Cu(L1)(Py)Cl]·H2O 1b, [Cu(L2)(Py)Cl] 2b, and [Cu(L2)(Py)NO3] 3b), where L1 = (E)-N'-(2-hydroxybenzylidene)acetohydrazide, L2 = (E)-N'-(2- hydroxybenzylidene)benzohydrazide, and Py = pyridine. All six Cu(II) complexes were assessed for their in vitro anticancer properties against a panel of human cancer cells, including cisplatin-resistant A549cisR cell lines. Interestingly, we observed that the 1:1:1 Cu/ligand/co-ligand mixed-ligand Cu(II) complexes exhibited higher anticancer activity than the corresponding 1:1 Cu(II)/ligand complexes. In particular, the 1:1:1 Cu(II)/ligand/co-ligand complex 3b displayed the greatest toxicity toward several cancer cells with better IC50 (1.12-3.77 μM) than cisplatin. Further mechanistic explorations showed that the 3b complex induced DNA damage, thus resulting in mitochondria-mediated apoptot...Continue Reading

Citations

Jul 4, 2019·Metallomics : Integrated Biometal Science·Ping YuFeng Yang
Oct 28, 2019·Metallomics : Integrated Biometal Science·Xiyu MoFupei Liang
Jun 4, 2020·International Journal of Molecular Sciences·Olga KrasnovskayaAlexander Majouga
Oct 4, 2020·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Simona RubinoIvana Pibiri
Jan 14, 2022·Dalton Transactions : an International Journal of Inorganic Chemistry·Yun-Qiong GuZhen-Feng Chen

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