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

Robillard, Marc S.; Jansen, Bart A. J.; Lochner, Martin; Geneste, Hervé; Li, Yi; Brouwer, Jaap; Hesse, Manfred; Reedijk, Jan (2001). Mononuclear Tetraamineplatinum(II) Complexes: Synthesis, Anticancer Activity, DNA Binding, and Cellular Uptake. Helvetica chimica acta, 84(10), pp. 3023-3030. Verlag Helvetica Chimica Acta 10.1002/1522-2675(20011017)84:10<3023::AID-HLCA3023>3.0.CO;2-Z

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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.

Item Type:

Journal Article (Original Article)

Division/Institute:

08 Faculty of Science > Departement of Chemistry and Biochemistry

UniBE Contributor:

Lochner, Martin

Subjects:

500 Science > 570 Life sciences; biology
500 Science > 540 Chemistry

ISSN:

0018-019X

Publisher:

Verlag Helvetica Chimica Acta

Language:

English

Submitter:

Martin Lochner

Date Deposited:

19 Dec 2014 11:01

Last Modified:

19 Dec 2014 11:01

Publisher DOI:

10.1002/1522-2675(20011017)84:10<3023::AID-HLCA3023>3.0.CO;2-Z

BORIS DOI:

10.7892/boris.60962

URI:

https://boris.unibe.ch/id/eprint/60962

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