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Mechanistic and Cytotoxicity Studies of Group IV b-Diketonate Complexes
Lord, Rianne M. Mannion, J.J. Hebden, A.J. Nako, A.E. Crossley, B.D. McMullon, M.W. Janeway, F.D. Phillips, Roger M. McGowan, P.C.
Lord, Rianne M.
Mannion, J.J.
Hebden, A.J.
Nako, A.E.
Crossley, B.D.
McMullon, M.W.
Janeway, F.D.
Phillips, Roger M.
McGowan, P.C.
Publication Date
2014-06
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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 b-diketonate coordination
complexes. Clear evidence that the ligands are exchangeable
on the metal centre and that the b-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 b-diketonate hafnium complex exhibiting
IC50 values of 4.9 0.9 mm and 3.2 0.3 mm against HT-29
and MCF-7, respectively, which are comparable with the activity
of cisplatin against the same cell lines. This tri b-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.
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Lord RM, Mannion JJ, Hebden AJ, Nako AE, Crossley BD, McMullon MW, Janeway FD, Phillips RM and McGowan PC (2014) Mechanistic and Cytotoxicity Studies of Group IV
b-Diketonate Complexes. ChemMedChem. 9(6): 1136–1139.
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