Fengfan Liu, Zhiping Zhou, S. Gou
Aug 5, 2014
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Journal
Journal of Coordination Chemistry
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. Graphical Abstract Three new platinum(II) complexes with 2-substituted malonate derivatives as leaving groups have been designed, synthesized, and spectrally characterized. They were tested in vitro against four human cancer cell lines. In addition, the DNA unwinding capability was also investigated.