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Electrochemical studies and potential anticancer activity in ferrocene derivatives

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posted on 2016-11-04, 09:08 authored by Sara Realista, Susana Quintal, Paulo N. Martinho, Ana I. Melato, Adrià Gil, Teresa Esteves, Maria de Deus Carvalho, Liliana P. Ferreira, Pedro D. Vaz, Maria José Calhorda

Several ferrocene derivatives (five mononuclear and two binuclear), including the new N-(p-chlorophenyl)-carboxamidoferrocene (1), were synthesized and their anticancer activity investigated. Two of them, 3 and 7, bearing a benzimidazole backbone were the most active against HeLa cells achieving IC50 values of ~5 μM along with 4 with a dipyridylamine ligand (~6 μM). Complex 6, also with a benzimidazole backbone, displayed slightly higher values (~11 μM). Cyclic voltammetry studies show that while the non-cytotoxic ferrocene derivatives 1, 2, and 5 follow a ferrocene-based redox behavior, derivatives 3, 4, 6, and 7 exhibit a more complex mechanism. These complex mechanisms are consistent with a more effective cytotoxic activity. Mössbauer spectroscopy parameters reflect a very small influence of the substituents.

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