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Novel platinum(IV) complexes induce rapid tumor cell death in vitro

2005; Wiley; Volume: 116; Issue: 3 Linguagem: Inglês

10.1002/ijc.21080

1097-0215

Goran Kaludjerovic, Djordje Miljković, Miljana Momčilović, V.M. Djinović, Marija Mostarica Stojković, Tibor J. Sabo, Vladimir Trajkovič,

Synthesis of Tetrazole Derivatives

The anticancer activity of platinum complexes has been known since the discovery of classical Pt(II)-based drug cisplatin. However, Pt(IV) complexes have greater inertness than corresponding Pt(II) complexes, thus allowing the oral administration and reducing the toxicity associated with platinum-based chemotherapy. Here, we describe the in vitro antitumor activity of some novel Pt(IV)-based agents against mouse fibrosarcoma L929 cells and human astrocytoma U251 cells. The cytotoxicity of 2 Pt(IV) complexes with bidentate ethylenediamine-N,N'-di-3-propanoato esters was found to be markedly higher than that of their Pt(II) counterparts and comparable to the antitumor action of cisplatin. In contrast to cisplatin, which caused oxidative stress-independent apoptotic cell death of tumor cells, these Pt(IV) complexes induced oxygen radical-mediated tumor cell necrosis. Importantly, the cytotoxic action of novel Pt(IV) complexes was markedly more rapid than that of cisplatin, indicating their potential usefulness in anticancer therapy.