Premium
β‐Ketoiminato Iridium(III) Organometallic Complexes: Selective Cytotoxicity towards Colorectal Cancer Cells HCT116 p53 ‐/‐
Author(s) -
Lord Rianne M.,
Zegke Markus,
Henderson Imogen R.,
Pask Christopher M.,
Shepherd Helena J.,
McGowan Patrick C.
Publication year - 2019
Publication title -
chemistry – a european journal
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.687
H-Index - 242
eISSN - 1521-3765
pISSN - 0947-6539
DOI - 10.1002/chem.201804901
Subject(s) - cytotoxicity , iridium , cisplatin , chemistry , colorectal cancer , cancer research , selectivity , cell culture , cancer , group 2 organometallic chemistry , mutant , cell , in vitro , stereochemistry , biochemistry , gene , biology , medicine , chemotherapy , catalysis , genetics , organic chemistry , molecule
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.