[摘要]：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, H-1 and C-13 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. LD50 was found to be 115 mg/kg by iv administration to ICR mice, much larger than that of oxaliplatin (LD50 = 19 mg/kg). (C) 2012 Elsevier Ltd. All rights reserved.
