Universität zu Köln

Lord, Rianne M., Zegke, Markus, Henderson, Imogen R., Pask, Christopher M., Shepherd, Helena J. and McGowan, Patrick C. (2019). beta-Ketoiminato Iridium(III) Organometallic Complexes: Selective Cytotoxicity towards Colorectal Cancer Cells HCT116 p53-/-. Chem.-Eur. J., 25 (2). S. 495 - 501. WEINHEIM: WILEY-V C H VERLAG GMBH. ISSN 1521-3765

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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 beta-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:	Journal Article
Creators:	Creators Email ORCID ORCID Put Code Lord, Rianne M. UNSPECIFIED UNSPECIFIED UNSPECIFIED Zegke, Markus UNSPECIFIED UNSPECIFIED UNSPECIFIED Henderson, Imogen R. UNSPECIFIED UNSPECIFIED UNSPECIFIED Pask, Christopher M. UNSPECIFIED UNSPECIFIED UNSPECIFIED Shepherd, Helena J. UNSPECIFIED UNSPECIFIED UNSPECIFIED McGowan, Patrick C. UNSPECIFIED UNSPECIFIED UNSPECIFIED
URN:	urn:nbn:de:hbz:38-159445
DOI:	10.1002/chem.201804901
Journal or Publication Title:	Chem.-Eur. J.
Volume:	25
Number:	2
Page Range:	S. 495 - 501
Date:	2019
Publisher:	WILEY-V C H VERLAG GMBH
Place of Publication:	WEINHEIM
ISSN:	1521-3765
Language:	English
Faculty:	Unspecified
Divisions:	Unspecified
Subjects:	no entry
Uncontrolled Keywords:	Keywords Language THIOREDOXIN REDUCTASE; ANTICANCER COMPLEXES; PLATINUM; MECHANISMS; EXPRESSION; THERAPY Multiple languages Chemistry, Multidisciplinary Multiple languages
Refereed:	Yes
URI:	http://kups.ub.uni-koeln.de/id/eprint/15944