Mononuclear Tetraamineplatinum(II) Complexes: Synthesis, Anticancer Activity, DNA Binding, and Cellular Uptake

The synthesis of three bis[(tert‐butoxy)carbonyl]‐protected (tetramine)dichloroplatinum complexes 2a – c of formula cis‐[PtCl2(LL)] and of their cationic deprotected analogs 3a – c and their evaluation with respect to in vitro cytotoxicity, intramolecular stability, DNA binding, and cellular uptake...

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Bibliographic Details
Published in:Helvetica chimica acta 2001-10, Vol.84 (10), p.3023-3030
Main Authors: Robillard, Marc S., Jansen, Bart A. J., Lochner, Martin, Geneste, Hervé, Li, Yi, Brouwer, Jaap, Hesse, Manfred, Reedijk, Jan
Format: Article
Language:English
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Summary:The synthesis of three bis[(tert‐butoxy)carbonyl]‐protected (tetramine)dichloroplatinum complexes 2a – c of formula cis‐[PtCl2(LL)] and of their cationic deprotected analogs 3a – c and their evaluation with respect to in vitro cytotoxicity, intramolecular stability, DNA binding, and cellular uptake is reported. The synthesis comprises the complexation of K2[PtCl4] with di‐N‐protected tetramines 1a – c to give 2a – c and subsequent acidolysis, yielding 3a – c. The cytotoxicity of the complexes is in direct relation to the length of the polyamine. Complexes 3a – c display a significant higher affinity for CT DNA as well as for cellular DNA in A2780 cells than cisplatin.
ISSN:0018-019X
1522-2675
DOI:10.1002/1522-2675(20011017)84:10<3023::AID-HLCA3023>3.0.CO;2-Z