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Enhancing the cellular uptake and antiproliferative activity of Ru(II) complexes using thermosensitive Diels-Alder cycloadditions

Haghdoost, Mohammad Mehdi; Poulet, Sylvain; Castonguay, Annie . Enhancing the cellular uptake and antiproliferative activity of Ru(II) complexes using thermosensitive Diels-Alder cycloadditions In: Inorganic Discussion Weekend (IDW), Novembre 3rd-5th 2017, Toronto.

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Résumé

Various stimuli-responsive strategies hold promise for the development of drug delivery systems that can efficiently overcome multiple obstacles associated with the treatment of cancer [1]. For instance, thermosensitive linkages such as Diels-Alder cycloadditions have the potential to offer simple and powerful tools for this purpose but have so far only scarcely been examined. Given the fact that furan moieties are commonly found in nature and are part of the structure of various therapeutics, it is of great interest to investigate drug delivery systems based on the Diels-Alder cycloaddition between furan-bearing anticancer drugs and molecules/platforms that contain dienophiles (such as maleimide moieties), as well as their retro Diels-Alder disassembly at physiological conditions. In this presentation, the synthesis and characterization of a promising class of anticancer metallic compounds, notably Ru(II)-arene complexes [2], and the influence brought about the introduction of a furan in their structure on their cancer cell antiproliferative activity will be discussed. However, the focus of the presentation will be on the unique ability of furan-containing ruthenium complexes to react with maleimide-modified agents via furan-maleimide Diels-Alder cycloadditions, as well as the impact of these linkages on the cellular uptake and antiproliferative activity of the complexes. Moreover, thermally-triggered retro Diels-Alder reactions, leading to the disassembly of Diels-Alder adducts and consequently the release of ruthenium complexes under biologically relevant conditions, will be discussed.

Type de document: Document issu d'une conférence ou d'un atelier
Mots-clés libres: -
Centre: Centre INRS-Institut Armand Frappier
Date de dépôt: 10 sept. 2018 20:42
Dernière modification: 10 sept. 2018 20:42
URI: http://espace.inrs.ca/id/eprint/7514

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