Lord, RM, Mannion, JJ, Hebden, AJ et al. (6 more authors) (2014) Mechanistic and cytotoxicity studies of group IV β-diketonate complexes. ChemMedChem, 9 (6). 1136 - 1139. ISSN 1860-7179
Abstract
Group IV metal complexes have previously shown promise as novel anticancer agents. Here, we discuss the mechanistic and cytotoxic nature of a series of group IV β-diketonate coordination complexes. Clear evidence that the ligands are exchangeable on the metal centre and that the β-diketonate ligands can act as potential drug delivery vehicles of the group IV metal ions was obtained. When evaluated for the cytotoxicity against human colon adenocarcinoma (HT-29) and human breast adenocarcinoma (MCF-7) cell lines, a general trend of decreasing potency down the group IV metals was observed. The most promising results obtained were for the hafnium complexes, with the tris diphenyl β-diketonate hafnium complex exhibiting IC50 values of 4.9 ± 0.9 μM and 3.2 ± 0.3 μM against HT-29 and MCF-7, respectively, which are comparable with the activity of cisplatin against the same cell lines. This tri β-diketonate hafnium complex is the first to show potent in vitro cytotoxic activity. The results reported show that ligand design has a significant effect on the cytotoxic potential of the complexes, and that these group IV complexes warrant further evaluation as novel metal-containing anticancer agents.
Metadata
Item Type: | Article |
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Authors/Creators: |
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Keywords: | anticancer agents; cytotoxicity; group IV; metal complexes; metals in medicine; Antineoplastic Agents; Apoptosis; Cisplatin; Coordination Complexes; Crystallography, X-Ray; Drug Screening Assays, Antitumor; HT29 Cells; Hafnium; Humans; Isomerism; MCF-7 Cells; Molecular Conformation |
Dates: |
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Institution: | The University of Leeds |
Academic Units: | The University of Leeds > Faculty of Engineering & Physical Sciences (Leeds) > School of Chemistry (Leeds) The University of Leeds > Faculty of Arts, Humanities and Cultures (Leeds) > School of Design (Leeds) |
Depositing User: | Symplectic Publications |
Date Deposited: | 11 Feb 2015 13:55 |
Last Modified: | 11 Feb 2015 13:55 |
Published Version: | http://dx.doi.org/10.1002/cmdc.201402019 |
Status: | Published |
Publisher: | Wiley-VCH Verlag |
Identification Number: | 10.1002/cmdc.201402019 |
Related URLs: | |
Open Archives Initiative ID (OAI ID): | oai:eprints.whiterose.ac.uk:82876 |