Antitumor and DNA-binding properties of a group of oligomeric complexes of Pt(II) and Pt(IV)

A. Peritz, S. Al-Baker, J. F. Vollano, J. E. Schurig, W. T. Bradner, J. C. Dabrowiak

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Abstract

The natitumor and DNA-binding properties of a group of oligomeric platinum(II) and platinum(IV) complexes are described. The compounds, having the stoichiometry [cis-Pt(II)(X)2(μ-OH)]2(NO3)2, where X is NH3, NH2 CH2CH3, and NH2CH(CH3)2, were found to be inactive or only weakly active against L-1210 leukemia. In vitro studies involving PM2-DNA show that these compounds bind to and unwind closed circular DNA in a manner similar to cis-Pt(II)(NH3)2Cl2. The Pt(IV) complexes produced by hydrogen peroxide oxidation of the Pt(II) dimers are inactive as antitumor agents and are incapable of unwinding PM2-DNA. The cyclotrimer [cis-Pt(II)(RR-DACH)(μ-OH)]3(NO3)3, where RR-DACH is (R,R)-1,2 diaminocyclohexane, exhibits potent antitumor activity against L-1210 leukemia and modest activities with B-16 and M5076 tumor lines. This compound platinates DNA, causing DNA unwinding and mobility shifts.

Original languageEnglish (US)
Pages (from-to)2184-2188
Number of pages5
JournalJournal of Medicinal Chemistry
Volume33
Issue number8
DOIs
StatePublished - 1990

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ASJC Scopus subject areas

  • Organic Chemistry

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Peritz, A., Al-Baker, S., Vollano, J. F., Schurig, J. E., Bradner, W. T., & Dabrowiak, J. C. (1990). Antitumor and DNA-binding properties of a group of oligomeric complexes of Pt(II) and Pt(IV). Journal of Medicinal Chemistry, 33(8), 2184-2188. https://doi.org/10.1021/jm00170a022