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

The synthesis and chemical characterization of two new trans platinum complexes, trans‐[PtCl2NH3(4‐hydroxymethylpyridine)] (1) and trans‐[PtCl4NH3(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‐[PtCl4NH3(4‐hydroxymethylpyridine)] were tested. Circular dichroism, 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‐[PtCl2NH3(4‐hydroxymethylpyridine)] than for trans‐[PtCl4NH3(4‐hydroxymethylpyridine)]. Complex 1 presents similar behavior to cisplatin, but with a lower IC50 at 24 h. Complex 1 also showed high apoptosis induction.

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