A series of 1
H
-benzo[
f
]chromene moieties (
4a–z
) were synthesised under Ultrasonic irradiation and confirmed with spectral analyses. Derivative
4i
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
4b–d
,
4k
,
4n
,
4q
, and
4w
, which possessed good potency against MCF-7/ADR, were tested as permeability glycoprotein (
P-
glycoprotein [
P
-gp]) expression inhibitors. The attained data confirmed that
4b–d
,
4q
, and
4w
exhibited strong expression inhibition against the
P-
gp alongside its cytotoxic effect on MCF-7/ADR. The western blot results and Rho123 accumulation assays showed that compounds
4b–d, 4q
, and
4w
effectively inhibited the
P
-gp expression and efflux function. Meanwhile,
4b–d
,
4q
, and
4w
induced apoptosis and accumulation of the treated MCF-7/ADR cells in the G1 phase and
4k
and
4n
in the S phase of the cell cycle.
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