期刊
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
卷 19, 期 11, 页码 -出版社
MDPI
DOI: 10.3390/ijms19113472
关键词
antitumoral activity; platinum; N-Heterocyclic carbene; polyethyleneimine
资金
- La Ligue Contre le Cancer-Grand-Est
- University of Strasbourg/CNRS-Program IDEX Interdisciplinaire
- French Ministere de la Recherche
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.
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