Abstract
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.