Synthesis, Characterization and Biological Evaluation of Platinum(II) Complexes with a Chiral N-Monosubstituted 1,2-Cyclohexyldiamine Derivative

摘要

Eight platinum(II) compounds with a new chiral ligand, 2-(((1 R ,2 R )-2-aminocyclohexylamino)methyl)phenol (HL), were designed, prepared and spectrally characterized. All compounds showed better aqueous solubility than cisplatin and oxaliplatin. In vitro cytotoxicity of these compounds against human HepG-2, MCF-7, A549 and HCT-116 cell lines was evaluated. Results indicated that all compounds showed cytotoxicity against A549 and HepG-2 cell lines. Particularly, compounds B1 and B8, which have CF₃SO₃? and (CH₃)₃COCH₂COO? as leaving groups, respectively, exhibited better cytotoxicitiy than that of carboplatin in these two cell lines.