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Synthesis, Characterization and Cytotoxicity of Ammine/Methylamine Platinum(Ⅱ) Complexes with Carboxylates

Synthesis, Characterization and Cytotoxicity of Ammine/Methylamine Platinum(Ⅱ) Complexes with Carboxylates
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摘要 Seven novel platinum (Ⅱ) complexes [ Pt(Ⅱ) (NH3) (CH3NH2)X2] (Ⅰ-Ⅶ ) ( X: CH3COO^-, CH2CICOO^- , CHCI2COO^- , C6H5-COO^- , p-CH3O--C6H4-COO^- , p-NH2-C6H4-COO^- , p-NO2--C6H4- COO^-) were prepared and characterized by means of elemental analysis, molar conductivity, thermal analysis, IR, UV, and ^1H NMR spectrometries. The cytotoxicity against HCT-8, BGC-823, MCF-7, EJ, and HL-60 cell lines increases in the following sequence: cisplatin 〉 Ⅳ 〉 Ⅴ 〉 Ⅵ 〉 Ⅶ 〉 Ⅰ 〉 Ⅱ 〉 Ⅲ. Moreover, the complexes ( Ⅰ --Ⅻ) display substantially greater activities agaist EJ and HL-60 cell lines than those against the cell lines from other carcinomas. They can induce a concentration-dependent accumulation of HL-60 cells in the G2/M phase of the cell cycle as cisplatin. There is no significant correlation between total DNA platination levels and cytotoxicity of the complexes. Seven novel platinum (Ⅱ) complexes [ Pt(Ⅱ) (NH3) (CH3NH2)X2] (Ⅰ-Ⅶ ) ( X: CH3COO^-, CH2CICOO^- , CHCI2COO^- , C6H5-COO^- , p-CH3O--C6H4-COO^- , p-NH2-C6H4-COO^- , p-NO2--C6H4- COO^-) were prepared and characterized by means of elemental analysis, molar conductivity, thermal analysis, IR, UV, and ^1H NMR spectrometries. The cytotoxicity against HCT-8, BGC-823, MCF-7, EJ, and HL-60 cell lines increases in the following sequence: cisplatin 〉 Ⅳ 〉 Ⅴ 〉 Ⅵ 〉 Ⅶ 〉 Ⅰ 〉 Ⅱ 〉 Ⅲ. Moreover, the complexes ( Ⅰ --Ⅻ) display substantially greater activities agaist EJ and HL-60 cell lines than those against the cell lines from other carcinomas. They can induce a concentration-dependent accumulation of HL-60 cells in the G2/M phase of the cell cycle as cisplatin. There is no significant correlation between total DNA platination levels and cytotoxicity of the complexes.
出处 《Chemical Research in Chinese Universities》 SCIE CAS CSCD 2006年第3期278-282,共5页 高等学校化学研究(英文版)
关键词 Ammine/methylamine platinum(Ⅱ) complex SYNTHESIS CYTOTOXICITY Cell cycle: DNA-binding Ammine/methylamine platinum(Ⅱ) complex Synthesis Cytotoxicity Cell cycle: DNA-binding
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