✦ LIBER ✦

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

✍ Scribed by Jean-Pierre Macquet; Theophile Theophanides

Publisher: Elsevier Science
Year: 1975
Weight: 434 KB
Volume: 5
Category: Article
ISSN: 0006-3061
DOI: 10.1016/s0006-3061(00)80221-5

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✦ Synopsis

In the present study the nature and the hydrolysis of DNA-I% complexes with the platinum compounds, [Pt(dien)C1]Cl, Imns-and ~rlrPt(NH~),Ci,, using potentiometric chloride determinations, have been investigated. The tmns-Pt(NH,),C1, and the [Pt(dien)Cl] Cl react with the GC planes at the N,(G) sites, while the cir-Pt(NH,),C& compound reacts with the CC planes and forms a chelate by using the N,(G) and O,(G) sites. The compIex is a specific 1:l Pt:DNA adduct. The platinum atom in &Pt(NH,),C1, liberates both chlorine atoms on chelation. A mechanism for the in vivo antitumor activity of the c&Pt(NH,),CI, is proposed and the structure activity reIationship is discussed_

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