title: High antitumor activity of 5,7-dihalo-8-quinolinolato cerium complexes.
abstract: Three cerium complexes: [Ce(ClQ)4] (1) (H-ClQ=5,7-dichloro-8-hydroxylquinoline), [Ce(ClIQ)4]·CH2Cl2·0.5H2O (2) (H-ClIQ=5-chloro-7-iodo-8-hydroxylquinoline) and [Ce2(BrQ)4(H-BrQ)(H2O)3Cl2]·1.5H2O (3) (H-BrQ=5,7-dibromo-8-hydroxylquinoline) were synthesized. The structures of 1 and 2 are mononuclear whereas 3 has a binuclear structure. Compared with the H-ClQ, H-ClIQ and H-BrQ, complexes 1-3 exhibited significantly higher cytotoxicity (IC50=0.09-5.23 μM) to SK-OV-3 and BEL-7404, 1 and 2 exhibited higher cytotoxicity to NCI-H460. Most the complexes and ligands exhibited higher cytotoxicity than cisplatin. Complexes 1-3 are much more sensitive to SK-OV-3 than to human normal liver cell HL-7702. Their antitumor activities were achieved through cell apoptosis and arrest at G0/G1-phase. Studies on the binding properties of 1-3 to DNA indicate that intercalation is the most probable binding mode.
authors.affiliation: Guangxi Key Laboratory for the Chemistry and Molecular Engineering of Medicinal Resources, School of Chemistry and Pharmacy of Guangxi Normal University, Guilin 541004, PR China. Electronic address: chenzfubc@yahoo.com.
authors.forename: Zhen-Feng
authors.initials: ZF
authors.lastname: Chen
authors.forename: Jian-Hua
authors.initials: JH
authors.lastname: Wei
authors.forename: Yan-Cheng
authors.initials: YC
authors.lastname: Liu
authors.forename: Mei
authors.initials: M
authors.lastname: Liu
authors.forename: Yun-Qiong
authors.initials: YQ
authors.lastname: Gu
authors.forename: Ke-Bin
authors.initials: KB
authors.lastname: Huang
authors.forename: Meng
authors.initials: M
authors.lastname: Wang
authors.forename: Hong
authors.initials: H
authors.lastname: Liang
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D017209:Apoptosis / Q000187:drug effects; D001665:Binding Sites; D002453:Cell Cycle / Q000187:drug effects; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D002563:Cerium / Q000737:chemistry / Q000494:pharmacology*; D002945:Cisplatin / Q000737:chemistry / Q000494:pharmacology; D056831:Coordination Complexes / Q000138:chemical synthesis* / Q000737:chemistry; D004354:Drug Screening Assays, Antitumor; D006219:Halogens / Q000737:chemistry*; D006801:Humans; D020128:Inhibitory Concentration 50; D015394:Molecular Structure; D011804:Quinolines / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*
chemical_list: D000970:Antineoplastic Agents; D056831:Coordination Complexes; D006219:Halogens; D011804:Quinolines; D002563:Cerium; D002945:Cisplatin
keywords: 5,7-Dihalo-8-quinolinoline; Cerium complex; Crystal structure; Cytotoxicity; DNA binding