title: Synthesis and cytotoxicity of diam(m)ineplatinum(II) complexes with 2,2-bis(hydroxymethyl)malonate as the leaving group.
abstract: Six diam(m)ineplatinum(II) complexes with 2,2-bis(hydroxymethyl)malonate as the leaving group were synthesized and characterized by elemental analysis, FAB-MS, FT-IR, (1)H and (13)C NMR along with a single crystal X-ray diffraction for a representative compound. All the complexes were evaluated for the cytotoxicity against human cancer cell lines A549/ATCC, HT-29, SGC-7901. The activity is related to the nature of the am(m)ine ligand. cis-[Pt(II)(1R,2R-Diaminocyclohexane)·2,2-bis(hydroxymethyl)malonate] (complex 5) exhibits the greatest activity among those six complexes, and is even more active than its parent compound oxaliplatin. LD(50) was found to be 115 mg/kg by iv administration to ICR mice, much larger than that of oxaliplatin (LD(50)=19 mg/kg).
authors.affiliation: State Key Laboratory of Advanced Technologies for Platinum Metals, Kunming Institute of Precious Metals, Yunnan, China.
authors.forename: Yingjuan
authors.initials: Y
authors.lastname: Xing
authors.forename: Liguang
authors.initials: L
authors.lastname: Lou
authors.forename: Xizhu
authors.initials: X
authors.lastname: Chen
authors.forename: Qingsong
authors.initials: Q
authors.lastname: Ye
authors.forename: Yongping
authors.initials: Y
authors.lastname: Xu
authors.forename: Chengying
authors.initials: C
authors.lastname: Xie
authors.forename: Jing
authors.initials: J
authors.lastname: Jiang
authors.forename: Weiping
authors.initials: W
authors.lastname: Liu
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D045744:Cell Line, Tumor; D056831:Coordination Complexes / Q000138:chemical synthesis* / Q000494:pharmacology; D018360:Crystallography, X-Ray; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D020128:Inhibitory Concentration 50; D007928:Lethal Dose 50; D009682:Magnetic Resonance Spectroscopy; D008314:Malonates / Q000138:chemical synthesis* / Q000494:pharmacology; D051379:Mice; D008813:Mice, Inbred ICR; D009944:Organoplatinum Compounds / Q000494:pharmacology; D000077150:Oxaliplatin; D013329:Structure-Activity Relationship
chemical_list: D000970:Antineoplastic Agents; D056831:Coordination Complexes; D008314:Malonates; D009944:Organoplatinum Compounds; D000077150:Oxaliplatin