Cytotoxic evaluation of substituted azetopyrroloazepinones

Abstract

Azetopyrroloazepinones 1a-g were synthesized in six steps from 5,5-dimethyl-1,3-cyclohexanedione as starting material in good yields. These compounds were tested on five tumoral cell lines with the aim of elucidating the relationship between the substituents attached to the 3-phenyl ring and their cytotoxic activity. The results are inconclusive in regard to the relationship between the physicochemical properties of the substituents on the 3-phenyl group of azeto-pyrroloazepinones 1a-g and the inhibition of the growth in tumor cell lines. However, the results show a clear link between the presence of halogens on position 3- or 4- and the cytotoxicity of these compounds.