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    Anticancer activity, DNA binding and cell mechanistic studies of estrogen- functionalised Cu(II) complexes

    Barrett, Stephen and De Franco, Michele and Kellett, Andrew and Dempsey, Eithne and Marzano, Cristina and Erxleben, Andrea and Gandin, Valentina and Montagner, Diego (2019) Anticancer activity, DNA binding and cell mechanistic studies of estrogen- functionalised Cu(II) complexes. Journal of Biological Inorganic Chemistry, 25. pp. 49-60. ISSN 0949-8257

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    Four estrogen-functionalised copper complexes were synthesised and investigated as electrochemical active DNA binding and cleavage agents. These complexes strategically contain a biocompatible metal centre [Cu(II)], a planar aromatic ligand as DNA intercalative agent and an estradiol-derivative moiety which acts as delivery vector to target estrogen-receptor-positive (ER+) cancer cells. Cytotoxic activity was studied over a panel of estrogen-receptor-positive (ER+) and negative (ER−) human cancer cell lines by means of both 2D and 3D cell viability studies. The complexes showed high in vitro intercalative interaction with nuclear DNA and demonstrated to be strong DNA cleaving agents. This series of Cu compounds are potent anticancer agents with low and sub-micromolar IC50 values and the cellular uptake follows the lipophilicity order meaning that the internalisation mainly happened via passive difusion. Finally, the estrogen-complexes are involved in the cellular redox stress by stimulating the production of ROS (reactive oxygen species).

    Item Type: Article
    Keywords: Anticancer activity; DNA binding; cell mechanistic studies; estrogen; functionalised; Cu(II); complexes;
    Academic Unit: Faculty of Science and Engineering > Chemistry
    Item ID: 14999
    Identification Number:
    Depositing User: Diego Montagner
    Date Deposited: 09 Nov 2021 15:56
    Journal or Publication Title: Journal of Biological Inorganic Chemistry
    Publisher: Springer Verlag
    Refereed: Yes
    Use Licence: This item is available under a Creative Commons Attribution Non Commercial Share Alike Licence (CC BY-NC-SA). Details of this licence are available here

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