?-Ketoiminato iridium(III) organometallic complexes: Selective cytotoxicity towards colorectal cancer cells HCT116 p53-/-

Lord, Rianne and Zegke, Markus and Henderson, Imogen R. and Pask, Christopher M. and Shepherd, Helena J. and McGowan, Patrick C. (2019) ?-Ketoiminato iridium(III) organometallic complexes: Selective cytotoxicity towards colorectal cancer cells HCT116 p53-/-. Chemistry - A European Journal, 25 (2). pp. 495-500. ISSN 0947-6539. (doi:https://doi.org/10.1002/chem.201804901?) (Access to this publication is currently restricted. You may be able to access a copy if URLs are provided)

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Abstract

This report presents a new library of organometallic iridium(III) compounds of the type [Cp*IrCl(N,O)] (Cp* = pentamethylcyclopentadienyl and N,O = a functionalized ??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.

Item Type: Article
Uncontrolled keywords: Bioinorganic chemistry, cancer, colorectal cancer, iridium, organometallic
Subjects: Q Science > QD Chemistry
R Medicine
Divisions: Faculties > Sciences > School of Physical Sciences
Depositing User: Helena Shepherd
Date Deposited: 07 Nov 2018 12:46 UTC
Last Modified: 28 Feb 2019 10:36 UTC
Resource URI: https://kar.kent.ac.uk/id/eprint/69980 (The current URI for this page, for reference purposes)
Shepherd, Helena J.: https://orcid.org/0000-0003-0832-4475
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