title: Synthesis, cytotoxicity, induction of apoptosis, and interaction with DNA of dinuclear platinum(II) complexes.
abstract: Six dicarboxylato-bridged dinuclear platinum(II) complexes S1-S6, with a newly designed chiral ligand, 2-{[(1R,2R)-2-aminocyclohexyl]amino}propanoic acid (HL), were prepared and spectrally characterized. The in vitro cytotoxicity of all resulting platinum(II) complexes was evaluated against human HCT-116, MCF-7, and HepG-2 tumor cell lines. The results show that all compounds exhibit positive biological activity toward HCT-116 and MCF-7 cell lines, of which complexes S3, S4, and S5, with succinate and its derivatives as bridges, showing better activity than the positive controls. Moreover, double-dyeing flow cytometric resection experiments indicate that the target compounds inhibit tumor cell growth by inducing apoptosis; gel electrophoresis experiments demonstrate the compounds' ability to prompt pET22b plasmid DNA degradation in almost the same way as oxaliplatin.
authors.affiliation: Pharmaceutical Research Center, School of Chemistry and Chemical Engineering, Southeast University, Nanjing 211189 (China); Jiangsu Province Hi-Tech Key Laboratory for Biomedical Research, Southeast University, Nanjing 211189 (China).
authors.forename: Gang
authors.initials: G
authors.lastname: Xu
authors.forename: Chuanzhu
authors.initials: C
authors.lastname: Gao
authors.forename: Shaohua
authors.initials: S
authors.lastname: Gou
authors.forename: Zhe
authors.initials: Z
authors.lastname: Cao
mesh_terms: D000970:Antineoplastic Agents / Q000737:chemistry* / Q000494:pharmacology*; D017209:Apoptosis / Q000187:drug effects*; D004247:DNA / Q000378:metabolism; D004354:Drug Screening Assays, Antitumor; D045325:HCT116 Cells; D006801:Humans; D008024:Ligands; D061986:MCF-7 Cells; D009369:Neoplasms / Q000188:drug therapy; D009944:Organoplatinum Compounds / Q000737:chemistry* / Q000494:pharmacology*
chemical_list: D000970:Antineoplastic Agents; D008024:Ligands; D009944:Organoplatinum Compounds; D004247:DNA