DNA-platinum interactions in vitro with trans- and cis-Pt(NH3)2Cl2.
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.
D001665:Binding Sites; D055598:Chemical Phenomena; D002621:Chemistry; D002945:Cisplatin; D004247:DNA; D006868:Hydrolysis; D007536:Isomerism; D007700:Kinetics; D008968:Molecular Conformation
D004247:DNA; D002945:Cisplatin