Mononuclear tetraamineplatinum(II) complexes: Synthesis, anticancer activity, DNA binding, and cellular uptake

被引：0

作者：

Robillard, Marc S. ^{[1
]}

Jansen, Bart A. J. ^{[1
]}

Lochner, Martin ^{[2
]}

Geneste, Hervé ^{[2
]}

Li, Yi ^{[2
]}

Brouwer, Jaap ^{[1
]}

Hesse, Manfred ^{[2
]}

Reedijk, Jan ^{[1
]}

机构：

[1] Leiden Institute of Chemistry, P.O. Box 9502, NL-2300 RA Leiden, Netherlands

[2] Organisch-chemisches Institut, Universität Zürich, Winterthurerstrasse 190, CH-8057 Zürich, Switzerland

来源：

| 2001年 / Verlag Helvetica Chimica Acta AG卷 / 84期

关键词：

Amines - Complexation - DNA - Positive ions - Synthesis (chemical) - Toxicity - Tumors;

D O I：

10.1002/1522-2675(20011017)84:103.0.CO;2-Z

中图分类号：

学科分类号：

摘要：

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.

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