title: Two water-soluble copper(II) complexes: synthesis, characterization, DNA cleavage, protein binding activities and in vitro anticancer activity studies.
abstract: Two water-soluble ternary copper(II) complexes of [Cu(L)Cl](ClO4) (1) and [Cu(L)Br2] (2) (L=(2-((quinolin-8-ylimino)methyl)pyridine)) were prepared and characterized by various physico-chemical techniques. Both 1 and 2 were structurally characterized by X-ray crystallography. The crystal structures show the presence of a distorted square-pyramidal CuN3Cl2 (1) or CuN3Br2 (2) geometry in which Schiff-base L acts as a neutral tridentate ligand. Both complexes present intermolecular π-π stacking interactions between quinoline and pyridine rings. The interaction of two complexes with CT-DNA (calf thymus-DNA) and BSA (bovine serum albumin) was studied by means of various spectroscopy methods, which revealed that 1 and 2 could interact with CT-DNA through intercalation mode, and could quench the intrinsic fluorescence of BSA in a static quenching process. Furthermore, the competition experiment using Hoechst 33258 indicated that two complexes may bind to CT-DNA by a minor groove. DNA cleavage experiments indicate that the complexes exhibit efficient DNA cleavage activities without any external agents, and hydroxyl radical (HO) and singlet oxygen ((1)O2) may serve as the major cleavage active species. Notably, the in vitro cytotoxicity of the complexes on three human tumor cells lines (HeLa, MCF-7, and A549) demonstrates that two compounds have broad-spectrum antitumor activity with quite low IC50 ranges of 0.43-1.85μM. Based on the cell cycle experiments, 1 and 2 could delay or inhibit cell cycle progression through the S phase.
authors.affiliation: Department of Chemistry, Nankai University, Tianjin 300071, People's Republic of China; Tianjin Key Laboratory of Metal and Molecule Based Material Chemistry, Tianjin 300071, People's Republic of China; Key Laboratory of Advanced Energy Materials Chemistry (MOE), Tianjin 300071, People's Republic of China; Collaborative Innovation Center of Chemical Science and Engineering, Tianjin, People's Republic of China.
authors.forename: Jing
authors.initials: J
authors.lastname: Lu
authors.affiliation: Department of Chemistry, Nankai University, Tianjin 300071, People's Republic of China; Tianjin Key Laboratory of Metal and Molecule Based Material Chemistry, Tianjin 300071, People's Republic of China; Key Laboratory of Advanced Energy Materials Chemistry (MOE), Tianjin 300071, People's Republic of China; Collaborative Innovation Center of Chemical Science and Engineering, Tianjin, People's Republic of China.
authors.forename: Qian
authors.initials: Q
authors.lastname: Sun
authors.affiliation: Department of Chemistry, Nankai University, Tianjin 300071, People's Republic of China; Tianjin Key Laboratory of Metal and Molecule Based Material Chemistry, Tianjin 300071, People's Republic of China; Key Laboratory of Advanced Energy Materials Chemistry (MOE), Tianjin 300071, People's Republic of China; Collaborative Innovation Center of Chemical Science and Engineering, Tianjin, People's Republic of China.
authors.forename: Jun-Ling
authors.initials: JL
authors.lastname: Li
authors.affiliation: Department of Chemistry, Nankai University, Tianjin 300071, People's Republic of China; Tianjin Key Laboratory of Metal and Molecule Based Material Chemistry, Tianjin 300071, People's Republic of China; Key Laboratory of Advanced Energy Materials Chemistry (MOE), Tianjin 300071, People's Republic of China; Collaborative Innovation Center of Chemical Science and Engineering, Tianjin, People's Republic of China.
authors.forename: Lin
authors.initials: L
authors.lastname: Jiang
authors.affiliation: Department of Chemistry, Nankai University, Tianjin 300071, People's Republic of China; Tianjin Key Laboratory of Metal and Molecule Based Material Chemistry, Tianjin 300071, People's Republic of China; Key Laboratory of Advanced Energy Materials Chemistry (MOE), Tianjin 300071, People's Republic of China; Collaborative Innovation Center of Chemical Science and Engineering, Tianjin, People's Republic of China.
authors.forename: Wen
authors.initials: W
authors.lastname: Gu
authors.affiliation: Department of Chemistry, Nankai University, Tianjin 300071, People's Republic of China; Tianjin Key Laboratory of Metal and Molecule Based Material Chemistry, Tianjin 300071, People's Republic of China; Key Laboratory of Advanced Energy Materials Chemistry (MOE), Tianjin 300071, People's Republic of China; Collaborative Innovation Center of Chemical Science and Engineering, Tianjin, People's Republic of China. Electronic address: liuxin64@nankai.edu.cn.
authors.forename: Xin
authors.initials: X
authors.lastname: Liu
authors.affiliation: Department of Chemistry, Nankai University, Tianjin 300071, People's Republic of China; Tianjin Key Laboratory of Metal and Molecule Based Material Chemistry, Tianjin 300071, People's Republic of China; Key Laboratory of Advanced Energy Materials Chemistry (MOE), Tianjin 300071, People's Republic of China; Collaborative Innovation Center of Chemical Science and Engineering, Tianjin, People's Republic of China. Electronic address: tiant@nankai.edu.cn.
authors.forename: Jin-Lei
authors.initials: JL
authors.lastname: Tian
authors.affiliation: Department of Chemistry, Nankai University, Tianjin 300071, People's Republic of China; Tianjin Key Laboratory of Metal and Molecule Based Material Chemistry, Tianjin 300071, People's Republic of China; Key Laboratory of Advanced Energy Materials Chemistry (MOE), Tianjin 300071, People's Republic of China; Collaborative Innovation Center of Chemical Science and Engineering, Tianjin, People's Republic of China.
authors.forename: Shi-Ping
authors.initials: SP
authors.lastname: Yan
mesh_terms: D000970:Antineoplastic Agents / Q000008:administration & dosage / Q000737:chemistry; D017209:Apoptosis / Q000187:drug effects*; D056831:Coordination Complexes / Q000008:administration & dosage / Q000138:chemical synthesis / Q000737:chemistry*; D003300:Copper / Q000737:chemistry*; D018360:Crystallography, X-Ray; D053837:DNA Cleavage; D006367:HeLa Cells; D006801:Humans; D066298:In Vitro Techniques; D008024:Ligands; D015394:Molecular Structure; D011485:Protein Binding; D014867:Water / Q000737:chemistry
chemical_list: D000970:Antineoplastic Agents; D056831:Coordination Complexes; D008024:Ligands; D014867:Water; D003300:Copper
keywords: Chemical nuclease; Copper complex; Cytotoxicity; Quinoline ring; Water-soluble