Department of Pharmaceutical and Pharmacological Sciences, University of Padova, Via F. Marzolo 5, 35131 Padova, Italy.
Bioorg Med Chem. 2013 Nov 15;21(22):6965-72. doi: 10.1016/j.bmc.2013.09.025. Epub 2013 Sep 19.
A convenient synthetic route and the characterization of complexes trans-[PtCl2(L)(PPh3)] (L=Et2NH (2), (PhCH2)2NH (3), (HOCH2CH2)2NH) (4) are reported. The antiproliferative activity was evaluated on three human tumor cell lines. The investigation on the mechanism of action highlighted for the most active complex 4 the capacity to affect mitochondrial functions. In particular, both the induction of the mitochondrial permeability transition phenomenon and an aspecific membrane damage occurred, depending on concentration.
报告了一种方便的合成路线和配合物 trans-[PtCl2(L)(PPh3)]（L=Et2NH（2），（PhCH2）2NH（3），（HOCH2CH2）2NH）（4）的表征。对三种人肿瘤细胞系进行了抗增殖活性评价。对作用机制的研究表明，最活跃的复合物 4 能够影响线粒体功能。特别是，在浓度依赖的情况下，诱导了线粒体通透性转换现象和非特异性的膜损伤。
