Abstract

In this paper we summarize the work on the development of trans-platinum complexes as antitumor agents during the last 15 years. We review the structures and chemical properties of many ‘transplatin’ analogues, symmetric and asymmetric, containing wide range of ligands, e.g.: heterocyclic planar or nonplanar amines, aliphatic amines, iminoethers and phosphoric ligands, as well as polynuclear platinum complexes. We emphasize differences in the cytotoxic activity between the various trans-platinum structures in comparison to cisplatin and transplatin in cisplatin-sensitive as well as cisplatin-resistant cell lines. Whenever available, we also report in vivo antitumor activity. In addition, for some trans-platinum complexes we present interaction with DNA, cell uptake, level of cellular DNA platination and the ability of the complexes to induce apoptosis. Finally, we describe the general methods of synthesis of trans-platinum(II) and (IV) complexes.

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