Abstract
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.
Highlights
Due to their unique properties, metal ions are the subject of intensive research for the development of drugs against acute illness [1]
The success of cisplatin remains a motivation for the development of new platinum complexes displaying lower side effects [4,5]
We studied the local platinum concentration effect onto the biological activity and concluded method for the synthesis of conjugates [11,12]
Summary
Due to their unique properties, metal ions are the subject of intensive research for the development of drugs against acute illness [1]. The interest in metal-based drugs has essentially started with the discovery of the antiproliferative activity of cisplatin by Rosenberg, which is still the most widely used anticancer drug (Figure 1) [2]. Cancer treatment with cisplatin (and its derivatives such as oxaliplatin) is accompanied by various severe toxic side effects and in addition tumour resistance is a real concern that pushes chemists and biologists to develop alternative molecules [3]. The success of cisplatin remains a motivation for the development of new platinum complexes displaying lower side effects [4,5]. Positive preliminary results motivated research and development in this direction and recently many NHC-containing platinum compounds have shown high activity in vitro against various cancer cell lines with cytotoxicity significantly higher than cisplatin (Figure 1) [7,8,9]. The (pre)clinical development of these new molecules as anticancer agents still faces multiple challenges, including the clarification of their mode of action
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