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Easy Derivatisation of Group 10 N-Heterocyclic Carbene Complexes and In Vitro Evaluation of an Anticancer Oestradiol Conjugate

Authors

  • Dr. Edith Chardon,

    1. Institut de Physique et Chimie des Matériaux de Strasbourg, Université de Strasbourg-CNRS UMR7504, 23 rue du Loess, BP 43, 67034 Strasbourg (France)
    2. Institut Européen de Chimie et Biologie, Université de Bordeaux-CNRS UMR5248, 2 rue Robert Escarpit, 33607 Pessac (France)
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  • Dr. Gian Luigi Puleo,

    1. Institut de Physique et Chimie des Matériaux de Strasbourg, Université de Strasbourg-CNRS UMR7504, 23 rue du Loess, BP 43, 67034 Strasbourg (France)
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  • Georges Dahm,

    1. Institut de Physique et Chimie des Matériaux de Strasbourg, Université de Strasbourg-CNRS UMR7504, 23 rue du Loess, BP 43, 67034 Strasbourg (France)
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  • Prof. Sylvie Fournel,

    1. Laboratoire de Conception et d'Applications de Molécules Bioactives, Université de Strasbourg-CNRS UMR7199, Faculté de Pharmacie 74 route du Rhin, 67400 Illkirch (France)
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  • Dr. Gilles Guichard,

    Corresponding author
    1. Institut Européen de Chimie et Biologie, Université de Bordeaux-CNRS UMR5248, 2 rue Robert Escarpit, 33607 Pessac (France)
    • Institut Européen de Chimie et Biologie, Université de Bordeaux-CNRS UMR5248, 2 rue Robert Escarpit, 33607 Pessac (France)
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  • Dr. Stéphane Bellemin-Laponnaz

    Corresponding author
    1. Institut de Physique et Chimie des Matériaux de Strasbourg, Université de Strasbourg-CNRS UMR7504, 23 rue du Loess, BP 43, 67034 Strasbourg (France)
    • Institut de Physique et Chimie des Matériaux de Strasbourg, Université de Strasbourg-CNRS UMR7504, 23 rue du Loess, BP 43, 67034 Strasbourg (France)
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Abstract

In the search for novel metal-based pharmaceuticals, ruthenium-catalysed 1,3-dipolar cycloaddition is used to functionalise a series of palladium and platinum N-heterocyclic carbene complexes. This strategy was applied to the conjugation of amino acid, polyethylene glycol and oestradiol derivatives with the aim of enhancing chemical diversity and introducing specific features (e.g., water solubility, cell targeting). Antiproliferative activities of the different complexes were assayed against several cancer cell lines (KB, MCF7, HCT116, PC3, SKOV3, OVCAR8, HL60) and healthy cell lines (MRC5, VERO, EPC), which established their efficiency. The ease of the structural derivatisation thus renders these complexes attractive metal-based systems for the development of selective targeted metal-hybrid anticancer drugs.

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