科研之友
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摘要
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 -diketonate coordination complexes. Clear evidence that the ligands are exchangeable on the metal centre and that the -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 -diketonate hafnium complex exhibiting IC50 values of 4.9 +/- 0.9M and 3.2 +/- 0.3M against HT-29 and MCF-7, respectively, which are comparable with the activity of cisplatin against the same cell lines. This tri -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.
- 出版日期2014-6
