title: Antitumor platinum(II) complexes of N-cyclobutyl-1R,2R-diaminocyclohexane with dicarboxylates as leaving groups.
abstract: Four platinum(II) complexes of N-cyclobutyl-1R,2R-diaminocyclohexane with different bidentate dicarboxylates (1 oxalate, 2 malonate, 3 1,1-cyclobutanedicarboxylate and 4 3-hydroxy-1,1-cyclobutanedicarboxylate) as leaving groups were synthesized and characterized by elemental analyses, IR and (1)HNMR spectra together with ESI-MS spectroscopy. All complexes showed considerable cytotoxicity against the tested four human tumor cell lines including A549, HCT-116, HepG-2 and MCF-7. Especially, complex 4 showed good cytotoxicity against A549 (IC50=3.5μM) and HCT-116 (IC50=0.9μM) cancer cell lines. Moreover, complex 3 is the most effective agent among the tested compounds against MCF-7 cell line (IC50=1.1μM). The DNA binding behavior of both complexes 3 and 4, studied by agarose gel electrophoresis, revealed that they bound to DNA in almost the same way as cisplatin.
authors.affiliation: Pharmaceutical Research Center, School of Chemistry and Chemical Engineering, Southeast University, Nanjing 211189, Jiangsu, China; Jiangsu Province Hi-Tech Key Laboratory for Bio-Medical Research, Southeast University, Nanjing 211189, Jiangsu, China; State Key Laboratory of Analytical Chemistry for Life Science, Nanjing University, Nanjing 210093, Jiangsu, China.
authors.forename: Gang
authors.initials: G
authors.lastname: Xu
authors.affiliation: Pharmaceutical Research Center, School of Chemistry and Chemical Engineering, Southeast University, Nanjing 211189, Jiangsu, China; Jiangsu Province Hi-Tech Key Laboratory for Bio-Medical Research, Southeast University, Nanjing 211189, Jiangsu, China.
authors.forename: Jian
authors.initials: J
authors.lastname: Zhao
authors.affiliation: Pharmaceutical Research Center, School of Chemistry and Chemical Engineering, Southeast University, Nanjing 211189, Jiangsu, China; Jiangsu Province Hi-Tech Key Laboratory for Bio-Medical Research, Southeast University, Nanjing 211189, Jiangsu, China. Electronic address: sgou@seu.edu.cn.
authors.forename: Shaohua
authors.initials: S
authors.lastname: Gou
authors.affiliation: State Key Laboratory of Analytical Chemistry for Life Science, Nanjing University, Nanjing 210093, Jiangsu, China.
authors.forename: Jie
authors.initials: J
authors.lastname: Pang
mesh_terms: D000970:Antineoplastic Agents / Q000737:chemistry*; D002264:Carboxylic Acids / Q000737:chemistry*; D003510:Cyclohexanes / Q000737:chemistry*; D004354:Drug Screening Assays, Antitumor / Q000379:methods; D045325:HCT116 Cells; D056945:Hep G2 Cells; D006801:Humans; D061986:MCF-7 Cells; D009944:Organoplatinum Compounds / Q000737:chemistry*
chemical_list: D000970:Antineoplastic Agents; D002264:Carboxylic Acids; D003510:Cyclohexanes; D009944:Organoplatinum Compounds; C506365:Cyclohexane
keywords: Anticancer platinum(II) complexes; Cytotoxicity; DNA cleavage; N-Cyclobutyl-1R,2R-diaminocyclohexane