Synthesis and antiproliferative activity of (1R,2R)-N1-(2-butyl)-1,2-cyclohexanediamine platinum(II) complexes with malonate derivatives |
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Abstract: | Three new platinum(II) complexes of (1R,2R)-N1-(2-butyl)-1,2-cyclohexanediamine with malonate derivatives as leaving groups have been synthesized and spectrally characterized. They were tested in vitro against four human cancer cell lines. (1R,2R)-N1-(2-butyl)-1,2-cyclohexanediamine-N,N′](2-ethylmalonato-O,O′)platinum(II) turned out to be more active (IC50 = 4.65 μM) than oxaliplatin (IC50 = 6.55 μM) against the MCF-7 cell line and is superior to its parent complex, (1R,2R)-N1-(2-butyl)-1,2-cyclohexanediamine-N,N′](malonato-O,O′)platinum(II). In addition, agarose gel electrophoresis study revealed that the interaction of the complex with pET22b plasmid DNA had a different behavior from that of cisplatin or oxaliplatin. |
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Keywords: | Platinum(II) complexes Malonate derivatives Cytotoxicity DNA binding Antitumor |
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