Synthesis, characterization and biological evaluation of platinum(2) complexes with a chiral N-monosubstituted 1,2-cyclohexyldiamine derivative

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  • Gao Chuanzhu
    Pharmaceutical Research Center, School of Chemistry and Chemical Engineering, Southeast University
  • Gou Shaohua
    Jiangsu Province Hi-Tech Key Laboratory for Bio-Medical Research, Southeast University Pharmaceutical Research Center, School of Chemistry and Chemical Engineering, Southeast University
  • Xu Gang
    Jiangsu Province Hi-Tech Key Laboratory for Bio-Medical Research, Southeast University Pharmaceutical Research Center, School of Chemistry and Chemical Engineering, Southeast University

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

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Eight platinum(II) compounds with a new chiral ligand, 2-(((1R,2R)-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.

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