Synthesis,Characterization and Biological Activity of trans-Platinum(II) and trans-Platinum(IV) Complexes with 4-Hydroxymethylpyridine

摘要

The synthesis and chemical characterization of two new trans platinum complexes,trans-[PtCI_2NH_3(4-hydroxymethylpyridine)] (1) and trans-[PtCI_4NH_3(4-hydroxymethylpyridine)] (2) are described.Their ability to interact with 5'-GMP by themselves and in the presence of reducing agents in the case of trans-[PtCl_4NH_3(4-hydroxymethylpyridine)] were tested.Circular dichro-ism,electrophoretic mobility in agarose gel,and atomic force microscopy studies showed that the interaction of complex 1 with DNA is stronger than that of complex 2.Cytotoxicity tests against HL-60 tumor cells also showed higher activity for trans-[PtCI_2NH_3(4-hydroxymethylpyridine)] than for trans-[PtCI_4NH_3(4-hydroxymethylpyridine)].Complex 1 presents similar behavior to cisplatin,but with a lower IC_(50) at 24 h.Complex 1 also showed high apoptosis induction.