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Open AccessArticle

N-Heterocyclic Carbene-Polyethyleneimine (PEI) Platinum Complexes Inducing Human Cancer Cell Death: Polymer Carrier Impact

UMR 7199, Faculté de Pharmacie, Université de Strasbourg-CNRS, 74 Route du Rhin, BP 60024, 67401 Illkirch CEDEX, France
Institut de Physique et Chimie des Matériaux de Strasbourg, UMR 7504 CNRS-Université de Strasbourg, 23 rue du Loess, 67000 Strasbourg, France
Authors to whom correspondence should be addressed.
These authors contributed equally to this work.
Int. J. Mol. Sci. 2018, 19(11), 3472;
Received: 8 October 2018 / Revised: 30 October 2018 / Accepted: 2 November 2018 / Published: 5 November 2018
(This article belongs to the Special Issue Platinum-Based Anti-Tumor Drugs)
The high interest in N-Heterocyclic platinum carbene complexes in cancer research stems from their high cytotoxicity to human cancer cells, their stability, as well as their ease of functionalization. However, the development of these new molecules as anticancer agents still faces multiple challenges, in particular solubility in aqueous media. Here, we synthesized platinum-NHC bioconjugates that combine water-solubility and cytotoxicity by using polyethyleneimine as polymer carrier. We showed on 8 different types of cells that the activity of these conjugates is modulated by the size of the polymer and the overall density of metal ions onto polymer chains. Using HCT116 cells, the conjugates displayed an effective activity after only 45 min of exposure in vitro correlated with a quick uptake by the cells as shown by the use of various fluorescent-tagged derivatives. View Full-Text
Keywords: antitumoral activity; platinum; N-Heterocyclic carbene; polyethyleneimine antitumoral activity; platinum; N-Heterocyclic carbene; polyethyleneimine
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MDPI and ACS Style

Wantz, M.; Bouché, M.; Dahm, G.; Chekkat, N.; Fournel, S.; Bellemin-Laponnaz, S. N-Heterocyclic Carbene-Polyethyleneimine (PEI) Platinum Complexes Inducing Human Cancer Cell Death: Polymer Carrier Impact. Int. J. Mol. Sci. 2018, 19, 3472.

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