β‐Ketoiminato Iridium(III) Organometallic Complexes: Selective Cytotoxicity towards Colorectal Cancer Cells HCT116 <i>p53</i>‐/‐
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- Rianne M. Lord
- School of Chemistry and Biosciences University of Bradford Richmond Road Bradford BD7 1DP UK
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- Markus Zegke
- School of Chemistry and Biosciences University of Bradford Richmond Road Bradford BD7 1DP UK
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- Imogen R. Henderson
- School of Chemistry University of Leeds Woodhouse Lane Leeds LS2 9JT UK
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- Christopher M. Pask
- School of Chemistry University of Leeds Woodhouse Lane Leeds LS2 9JT UK
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- Helena J. Shepherd
- School of Chemistry University of Leeds Woodhouse Lane Leeds LS2 9JT UK
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- Patrick C. McGowan
- School of Chemistry University of Leeds Woodhouse Lane Leeds LS2 9JT UK
抄録
<jats:title>Abstract</jats:title><jats:p>This report presents a new library of organometallic iridium(III) compounds of the type [Cp*IrCl(<jats:italic>L</jats:italic>)] (Cp*=pentamethylcyclopentadienyl and <jats:italic>L</jats:italic>=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 <jats:italic>p53</jats:italic>‐null colorectal cell line, HCT116 <jats:italic>p53‐/</jats:italic>‐, 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 <jats:italic>p53</jats:italic> and has potential applications in treatment of cancers for which the <jats:italic>p53</jats:italic> gene is absent or mutant.</jats:p>
収録刊行物
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- Chemistry – A European Journal
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Chemistry – A European Journal 25 (2), 495-500, 2018-12-06
Wiley