Identification of some benzoxazepines as anticancer agents inducing cancer cell apoptosis.

Aim: Using cytotoxic agents with apoptosis induction may represent one of new strategies for cancer treatment to overcome the increased resistance of the disease.

Methodology: Two series of benzo[f][1,4]oxazepine-3,5(2H,4H)-diones (compounds 5, 6a-f) and 3-phenylbenzo[f][1,4]oxazepin-5(4H)-ones (compounds 10, 11a-f) were synthesized and screened for their cytotoxicity against leukemia K-562 and breast T-47D cancer cell lines as well as normal fibroblasts WI-38.

Results: The tested compounds revealed good cytotoxicity and selectivity toward cancer cell lines relative to the normal cells, especially compounds 6f, 10 and 11e, f.