Mechanistic and Cytotoxicity Studies of Group IV β-Diketonate Complexes

R.M. Lord, J.J. Mannion, A.J. Hebden, A.E. Nako, B.D. Crossley, M.W. McMullon, F.D. Janeway, R.M. Phillips, P.C. McGowan

Research output: Contribution to journalArticlepeer-review

18 Citations (Scopus)

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. 
Original languageEnglish
Pages (from-to)1136-1139
Number of pages4
JournalChemMedChem
Volume9
Issue number6
Early online date29 Apr 2014
DOIs
Publication statusPublished - 1 Jun 2014
Externally publishedYes

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