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    β‐Ketoiminato Iridium(III) Organometallic Complexes: Selective Cytotoxicity towards Colorectal Cancer Cells HCT116 p53‐/‐

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    Publication date
    2019-01-07
    Author
    Lord, Rianne M.
    Zegke, Markus
    Henderson, I.R.
    Pask, C.M.
    Shepherd, H.J.
    McGowan, P.C.
    Keyword
    Bioinorganic chemistry
    Cancer
    Colorectal cancer
    Iridium
    Organometallic
    Rights
    (c) 2019 Wiley. This is the peer-reviewed version of the following article: Lord RM, Zegke M, Henderson IR et al (2019) β‐Ketoiminato Iridium(III) Organometallic Complexes: Selective Cytotoxicity towards Colorectal Cancer Cells HCT116 p53‐/‐. Chemistry - A European Journal. 25(2): 495-500, which has been published in final form at https://doi.org/10.1002/chem.201804901. This article may be used for non-commercial purposes in accordance with Wiley Terms and Conditions for Self-Archiving
    Peer-Reviewed
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    Abstract
    This report presents a new library of organometallic iridium(III) compounds of the type [Cp*IrCl(L)] (Cp*=pentamethylcyclopentadienyl and L=a functionalized β‐ketoiminato ligand) showing moderate to high cytotoxicity against a range of cancer cell lines. All compounds show increased activity towards colorectal cancer, with preferential activity observed against the immortalized p53‐null colorectal cell line, HCT116 p53‐/‐, with sensitivity factors (SF) up to 26.7. Additionally, the compounds have excellent selectivity for cancerous cells when tested against normal cell types, with selectivity ratios (SR) up to 35.6, contrary to that of cisplatin, which is neither selective nor specific for cancerous cells (SF=0.43 and SR=0.7–2.3). This work provides a preliminary understanding of the cytotoxicity of iridium compounds in the absence of p53 and has potential applications in treatment of cancers for which the p53 gene is absent or mutant.
    URI
    http://hdl.handle.net/10454/16755
    Version
    Accepted Manuscript
    Citation
    Lord RM, Zegke M, Henderson IR et al (2019) β‐Ketoiminato Iridium(III) Organometallic Complexes: Selective Cytotoxicity towards Colorectal Cancer Cells HCT116 p53‐/‐. Chemistry - A European Journal. 25(2): 495-500.
    Link to publisher’s version
    https://doi.org/10.1002/chem.201804901
    Type
    Article
    Collections
    Life Sciences Publications

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