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    Synthesis, characterisation and in vitro antitumour potential of novel Pt(II) estrogen linked complexes

    Kitteringham, Eolann and Andriollo, Emma and Gandin, Valentina and Montagner, Diego and Griffity, Darren M. (2019) Synthesis, characterisation and in vitro antitumour potential of novel Pt(II) estrogen linked complexes. Inorganica Chimica Acta, 495 (118944). ISSN 0020-1693

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    The Cu(I) alkyne azide click reaction of 17α-ethynylestradiol and di-tert-butyl (2-azidopropane-1,3-diyl)dicarbamate afforded the novel 1,4 disubstituted 1,2,3 triazole and estrogen-based ligand 2-(4-(estradiol)-1H1,2,3-triazol-1-yl)propane-1,3-diamine, EDiolDap. Reaction of EDiolDap with Pt(II) DMSO precursors, cis- [PtCl2(DMSO)2] and cis-[Pt(CBDCA)(DMSO)2] gave the corresponding Pt(II) estrogen linked complexes [PtCl2(EDiolDap)] and [Pt(CBDCA)(EDiolDap)] respectively in good yield. Both Pt(II) estrogen linked complexes exhibited superior activity as compared to cisplatin and carboplatin in 2D culture and exhibited ca. 30 fold higher activity, in terms of IC50 values, against ER+ cancer cells (cervical, breast and ovarian) as compared to the reference ER− colon cancer line. [PtCl2(EDiolDap)] and [Pt(CBDCA)(EDiolDap)] retained their anti-tumour activity in an ovarian 3D spheroid culture model and reduced the viability of ovarian cancer cell spheroids ca. 9- fold and 5-fold better, respectively, as compared to cisplatin.

    Item Type: Article
    Additional Information: EK sincerely thanks the Royal College of Surgeons in Ireland for financial support through the RCSI Apjohn Scholarship. This publication has emanated from research supported in part by a research grant from Science Foundation Ireland (SFI) and is co-funded under the European Regional Development Fund under Grant Number 12/RC/ 2275_P2
    Keywords: Platinum; Steroid; Estradiol; Click chemistry; Triazole; In vitro cytotoxicity; Spheroid;
    Academic Unit: Faculty of Science and Engineering > Chemistry
    Item ID: 13920
    Identification Number:
    Depositing User: Diego Montagner
    Date Deposited: 02 Feb 2021 14:40
    Journal or Publication Title: Inorganica Chimica Acta
    Publisher: Elsevier
    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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