title: Preparation and Biological Evaluation of Two Novel Platinum(II) Complexes Based on the Ligands of Dipicolyamine Bisphosphonate Esters.
abstract: Two new platinum(II)-based complexes bearing a bone-targeting group were synthesized and characterized. They both have excellent affinity for hydroxyapatite (HA), which is abundant in human bone tissues. Their antitumor activities against five human cancer cell lines (U2OS, A549, HCT116, MDA-MB-231 and HepG2) were evaluated and compared with cisplatin (CDDP). Though the antitumor efficacies of new complexes are lower than that of CDDP, they show higher selectivity against the HepG2 hepatoma cell line than the L02 normal liver cell line. Morphology studies exhibited typical characteristics of cell apoptosis and the cell cycle distribution analysis indicated that the complexes can inhibit cancer cells by inducing cell cycle arrest at the G2/M phase, a similar mechanism of action to CDDP.
authors.affiliation: Jiangsu Key Laboratory of Molecular Nuclear Medicine, Key Laboratory of Nuclear Medicine, Ministry of Health, Jiangsu Institute of Nuclear Medicine, Wuxi 214063, China. qiuling@jsinm.org.
authors.forename: Ling
authors.initials: L
authors.lastname: Qiu
authors.affiliation: Jiangsu Key Laboratory of Molecular Nuclear Medicine, Key Laboratory of Nuclear Medicine, Ministry of Health, Jiangsu Institute of Nuclear Medicine, Wuxi 214063, China. lhgnsfxy@hotmail.com.
authors.forename: Hong
authors.initials: H
authors.lastname: Liu
authors.affiliation: Jiangsu Key Laboratory of Molecular Nuclear Medicine, Key Laboratory of Nuclear Medicine, Ministry of Health, Jiangsu Institute of Nuclear Medicine, Wuxi 214063, China. like@jsinm.org.
authors.forename: Ke
authors.initials: K
authors.lastname: Li
authors.affiliation: Jiangsu Key Laboratory of Molecular Nuclear Medicine, Key Laboratory of Nuclear Medicine, Ministry of Health, Jiangsu Institute of Nuclear Medicine, Wuxi 214063, China. lvgaochao@jsinm.org.
authors.forename: Gaochao
authors.initials: G
authors.lastname: Lv
authors.affiliation: Jiangsu Key Laboratory of Molecular Nuclear Medicine, Key Laboratory of Nuclear Medicine, Ministry of Health, Jiangsu Institute of Nuclear Medicine, Wuxi 214063, China. nmuyanghui@sina.com.
authors.forename: Hui
authors.initials: H
authors.lastname: Yang
authors.affiliation: Jiangsu Key Laboratory of Molecular Nuclear Medicine, Key Laboratory of Nuclear Medicine, Ministry of Health, Jiangsu Institute of Nuclear Medicine, Wuxi 214063, China. qinxiaofeng@jsinm.org.
authors.forename: Xiaofeng
authors.initials: X
authors.lastname: Qin
authors.affiliation: Jiangsu Key Laboratory of Molecular Nuclear Medicine, Key Laboratory of Nuclear Medicine, Ministry of Health, Jiangsu Institute of Nuclear Medicine, Wuxi 214063, China. linjianguo@jsinm.org.
authors.forename: Jianguo
authors.initials: J
authors.lastname: Lin
mesh_terms: D000327:Adsorption; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D017209:Apoptosis / Q000187:drug effects / Q000235:genetics; D001842:Bone and Bones / Q000737:chemistry; D002460:Cell Line; D045744:Cell Line, Tumor; D002945:Cisplatin / Q000494:pharmacology; D004164:Diphosphonates / Q000138:chemical synthesis* / Q000494:pharmacology; D004354:Drug Screening Assays, Antitumor; D017886:Durapatite / Q000737:chemistry*; D059565:G2 Phase Cell Cycle Checkpoints / Q000187:drug effects* / Q000235:genetics; D045325:HCT116 Cells; D056945:Hep G2 Cells; D006801:Humans; D020128:Inhibitory Concentration 50; D008956:Models, Chemical; D009928:Organ Specificity; D009944:Organoplatinum Compounds / Q000138:chemical synthesis* / Q000494:pharmacology
chemical_list: D000970:Antineoplastic Agents; D004164:Diphosphonates; D009944:Organoplatinum Compounds; D017886:Durapatite; D002945:Cisplatin
keywords: action mechanism; antitumor activity; dipicolyamine bisphosphonate ester; hydroxyapatite affinity; platinum complex