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Oxidation of anticancer Pt(Ⅱ) complexes with monodentate phosphane ligands: towards stable but active Pt(Ⅳ) prodrugs

机译:具有单齿膦配体的抗癌Pt(Ⅱ)配合物的氧化:趋向稳定但活性的Pt(Ⅳ)前药

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摘要

The synthesis, characterization and cytotoxicity studies of two novel platinum(Ⅳ) complexes, trans-PtCl_4(dma)(PPh_3), 1, and trans-PtCl_4(ipa)(PPh_3), 2, where dma is dimethylamine and ipa is iso-propylamine, have been carried out. Both complexes contain aliphatic amines trans to phosphane ligands as a good alternative to take advantage of the phosphane group lipophilicity and the stability of platinum(Ⅳ) to obtain more effective drugs. Moreover, the complexes are stable in solution and such stability allowed their antitumoral action and DNA interaction to be checked and proved.
机译:两种新型铂(Ⅳ)配合物,反式-PtCl_4(dma)(PPh_3),1和反式-PtCl_4(ipa)(PPh_3),2的合成,表征和细胞毒性研究,其中dma是二甲胺,ipa是iso-丙胺,已进行。两种配合物均含有反式膦配体的脂肪胺,可以很好地替代膦基的亲脂性和铂(Ⅳ)的稳定性,从而获得更有效的药物。此外,该复合物在溶液中是稳定的,并且这种稳定性允许检查和证明它们的抗肿瘤作用和DNA相互作用。

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