Add time:08/05/2019         Source:sciencedirect.com

Due to their inertness, platinum(IV) complexes are well known potential candidates to improve the pharmacological properties and selective cellular uptake of commonly used platinum(II) anticancer agents. In these 6-coordinate prodrugs, the equatorial nonleaving groups are the only ligands which remain in the final Pt-DNA adducts and directly affect the DNA binding property. In an effort to discover the structure–activity relationship; in this report, two novel platinum(IV) complexes, trans-[Pt(3phpy)2Cl4] (1) and [Pt(4dtb-bpy)Cl4].DMSO (2) (3phpy = 3-phenylpyridine and 4dtb-bpy = 4,4′-di-tert-butyl-2,2′-bipyridine) were prepared and fully characterized. Their in vitro activity was evaluated and compared with those of similar platinum(IV) complexes, containing unbranched ligands, trans-[Pt(py)2Cl4] and [Pt(bpy)Cl4]. Interestingly, complex 1, with phenylpyridine nonleaving ligands, demonstrated further antiproliferative properties among the studied platinum(IV) prodrugs. Moreover, the apoptosis rate in cell lines was also determined using flow cytometry. Furthermore, the resistance factor of complexes 1 and 2 were 1.1 and 1.3, respectively, using wild-type and cisplatin-resistant A2780 cell lines.

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