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DNA-platinum interactions in vitro with trans- and cis- Pt(NH3)2Cl2

1975; Elsevier BV; Volume: 5; Issue: 1 Linguagem: Inglês

10.1016/s0006-3061(00)80221-5

1873-3190

Jean-Pierre Macquet, Théophile Theophanides,

DNA and Nucleic Acid Chemistry

In the present study the nature and the hydrolysis of DNA-Pt complexes with the platinum compounds, [Pt(dien)Cl]Cl, trans- and cis-Pt(NH3)2Cl2, using potentiometric chloride determinations, have been investigated. The trans-Pt(NH3)2Cl2 and the [Pt(dien)Cl]Cl react with the GC planes at the N7(G) sites, while the cis-Pt(NH3)2Cl2 compound reacts with the GC planes and forms a chelate by using the N7(G) and O6(G) sites. The complex is a specific 1:1 Pt:DNA adduct. The platinum atom in cis-Pt(NH3)2Cl2 liberates both chlorine atoms on chelation. A mechanism for the in vivo antitumor activity of the cis-Pt(NH3)2Cl2 is proposed and the structure activity relationship is discussed.