?
Синтез, строение и цитотоксические свойства комплексов платины(IV), содержащих аминоксильные и дихлорацетатные лиганды
New platinum(IV)-aminoxyl complexes (PAC) 2a,b have been synthesized, containing aminoxyl radical with antioxidant properties in one of equatorial position, and axial ligands are represented by dichloroacetate, capable of inhibiting energy production through glycolysis in tumor cells. Complexes 2a,b are characterized by moderate lipophilicity (lg Pow ~2) and differ in the redox properties of aminoxyls. Cytotoxic properties of complexes 2a,b were studied in tumor (HeLa, HepG2, MCF-7) and non-tumor Vero cells in comparison with cisplatin (CP), satraplatin (JM216), as well as with PAC 3a,b containing axial acetate ligands. The cytotoxicity of complexes 2a,b against tumor cells (IC50 19-171 mkM) was 2-11 fold higher than that of complexes 3a,b and comparable to that of CP and JM216 (IC50 10-187 mkM). For Vero non–tumor cells, the cytotoxicity of 2a,b (IC50 62-124 mkM) was significantly lower than that of CP and JM216 (IC50 17.6-33 mkM).