Β‐Ketoiminato Iridium(III) Organometallic Complexes: Selective Cytotoxicity towards Colorectal Cancer Cells HCT116 p53‐/‐. Issue 2 (6th December 2018)

• Record Type: Journal Article
• Authors: Lord, Rianne M.; Zegke, Markus; Henderson, Imogen R.; Pask, Christopher M.; Shepherd, Helena J.; McGowan, Patrick C.
• Is Part Of: Chemistry. Volume 25:Issue 2(2019)
• Page Start: 495
• Page End: 500
• Publication Date: 2018-12-06
• Subjects: bioinorganic chemistry -- cancer -- colorectal cancer -- iridium -- organometallic; Chemistry -- Periodicals; 540
• DOI: 10.1002/chem.201804901
• Languages: English
• ISSNs: 0947-6539

Abstract

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. Abstract : Colorectal cancer selective iridium drugs : This work presents new organometallic iridium(III) compounds that are sensitive to colorectal cancer cells, especially those with null p53 genes. Additionally, they are selective towards cancer cells over normal cells, contrary to cisplatin, which is neither sensitive nor selective towards cancer (see figure).