Mechanistic and Cytotoxicity Studies of Group IV b-Diketonate Complexes

Autor: 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.
Jazyk: angličtina
Rok vydání: 2014
Předmět:
Druh dokumentu: Článek
DOI: 10.1002/cmdc.201402019
Popis: 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.
Databáze: Networked Digital Library of Theses & Dissertations