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Issue 48, 2009
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Non-traditional platinum compounds for improved accumulation, oral bioavailability, and tumor targeting

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Abstract

The five platinum anticancer compounds currently in clinical use conform to structure–activity relationships formulated (M. J. Cleare and J. D. Hoeschele, Bioinorg. Chem., 1973, 2, 187–210) shortly after the discovery that cis-diamminedichloroplatinum(II), cisplatin, has antitumor activity in mice. These compounds are neutral platinum(II) species with two am(m)ine ligands or one bidentate chelating diamine and two additional ligands that can be replaced by water through aquation reactions. The resulting cations ultimately form bifunctional adducts on DNA. Information about the chemistry of these platinum compounds and correlations of their structures with anticancer activity have provided guidance for the design of novel anticancer drug candidates based on the proposed mechanisms of action. This article discusses advances in the synthesis and evaluation of such non-traditional platinum compounds, including cationic and tumor-targeting constructs.

Graphical abstract: Non-traditional platinum compounds for improved accumulation, oral bioavailability, and tumor targeting

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Publication details

The article was received on 10 Jul 2009, accepted on 27 Aug 2009 and first published on 01 Oct 2009


Article type: Perspective
DOI: 10.1039/B913896J
Citation: Dalton Trans., 2009,0, 10651-10659
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    Non-traditional platinum compounds for improved accumulation, oral bioavailability, and tumor targeting

    K. S. Lovejoy and S. J. Lippard, Dalton Trans., 2009, 0, 10651
    DOI: 10.1039/B913896J

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