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β‐Ketoiminato Iridium(III) Organometallic Complexes: Selective Cytotoxicity towards Colorectal Cancer Cells HCT116 p53‐/‐
Lord, Rianne M. Zegke, Markus Henderson, I.R. Pask, C.M. Shepherd, H.J. McGowan, P.C.
Lord, Rianne M.
Zegke, Markus
Henderson, I.R.
Pask, C.M.
Shepherd, H.J.
McGowan, P.C.
Publication Date
2019-01-07
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(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
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2018-10-25
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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.
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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.
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Article