Synthesis and cytotoxic activity of [benzo[b][1,4]oxazepino[7,6,5-de]quinolin-2-yl]-1,3-tropolones

Abstract

We describe the synthesis of previously unknown halogenated derivatives of 2-(benzo[b][1,4]oxazepino[7,6,5-de]quinolin-2-yl)-1,3-tropolone. The MTT colorimetric assay was used to detect anticancer activity and inhibition of human epidermoid carcinoma (KB human epithelial carcinoma cell line) growth by 9,11-di(tert-butyl)-5-chloro-2,4-dimethyl-7Н-enzo[b][1,4]oxazepino[7,6,5-de]quinoline at IC50 93.7 μg/ml, and human breast carcinoma (MCF-7 cell line) growth by 2-[7-acetyl-9,11-di(tert-butyl)-5-chloro-4-methylbenzo[b][1,4]-oxazepino[7,6,5-de]quinolin-2-yl]-5,6,7-trichloro-1,3-tropolone at IC50 12.96 μg/ml.