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.

Synthesis of novel pyrroloazepinones by Schmidt expansions of 6-indolones

“…Pyrroloazepinones are biheterocyclic compounds that display an important diversity of biological properties, which have been used for the treatment of Alzheimer's, 1 arthritis and many types of cancer [2][3][4][5][6] (Scheme 1). They have been found in derivatives of natural products such as paullones 6 , hymenialdisine 1 , and stevensine 7 .…”