Discovery of benzochromene derivatives first example with dual cytotoxic activity against the resistant cancer cell MCF-7/ADR and inhibitory effect of the -glycoprotein expression levels.

A series of 1-benzo[]chromene moieties () were synthesised under Ultrasonic irradiation and confirmed with spectral analyses. Derivative solely possessed an X-ray single crystal. The anti-proliferative efficacy of the desired molecules has been explored against three cancer cells: MCF-7, HCT-116, and HepG-2 with the cytotoxically active derivatives screened against MCF-7/ADR and normal cells HFL-1 and WI-38. Furthermore, compounds , , , , and , which possessed good potency against MCF-7/ADR, were tested as permeability glycoprotein (glycoprotein [-gp]) expression inhibitors. The attained data confirmed that , , and exhibited strong expression inhibition against the gp alongside its cytotoxic effect on MCF-7/ADR. The western blot results and Rho123 accumulation assays showed that compounds , and effectively inhibited the -gp expression and efflux function. Meanwhile, , , and induced apoptosis and accumulation of the treated MCF-7/ADR cells in the G1 phase and and in the S phase of the cell cycle.