Novel platinum(II) complexes of long chain aliphatic diamine ligands with oxalato as the leaving group: comparative cytotoxic activity relative to chloride precursors

Journal of the Brazilian Chemical Society

Heveline Silva¹  Carolina V. Barra¹  Fillipe V. Rocha¹  Frederic Frézard²  Miriam T. P. Lopes²  Ana Paula S. Fontes¹ 

[1] ,Universidade Federal de Juiz de Fora Departamento de Química Juiz de Fora MG ,Brazil

关键词: ethylenediamine;    oxalato;    platinum;    complexes;    antitumor agents;   

DOI  :  10.1590/S0103-50532010001000023

来源: SciELO

【 摘 要 】

Platinum complexes play an important role in the development of anticancer drugs. Their cytotoxicity can be influenced by the nature of the leaving ligands, due to the hydrolysis reaction that occurs prior to the binding of the platinum complex to DNA. Also, non-leaving groups such as lipophilic diamines may affect cellular uptake. In this work, we describe the synthesis of platinum(II) complexes having oxalato and long chain aliphatic N-alkyl ethylenediamines as ligands. The products were characterized by elemental analyses, infrared spectroscopy and ¹H, 13C and 195Pt NMR spectroscopy. Biological activity was assessed against tumor cell lines (A549, B16-F1, B16-F10, MDA-MB-231) and non-tumor cell lines (BHK-21 and CHO). The length of the carbon chain affects the cytotoxicity and the oxalato complexes were less cytotoxic than the respective chloride-containing analogues.

【 授权许可】

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