Synthesis, Characterization, and Anticancer Activity of New Quinazoline Derivatives against MCF-7 Cells

Abstract EN

Two new synthesized and characterized quinazoline Schiff bases 1 and 2 were investigated for anticancer activity against MCF-7 human breast cancer cell line.

Compounds 1 and 2 demonstrated a remarkable antiproliferative effect, with an IC50 value of 6.246 × 10−6 mol/L and 5.910 × 10−6 mol/L, respectively, after 72 hours of treatment.

Most apoptosis morphological features in treated MCF-7 cells were observed by AO/PI staining.

The results of cell cycle analysis indicate that compounds did not induce S and M phase arrest in cell after 24 hours of treatment.

Furthermore, MCF-7 cells treated with 1 and 2 subjected to apoptosis death, as exhibited by perturbation of mitochondrial membrane potential and cytochrome c release as well as increase in ROS formation.

We also found activation of caspases-3/7, -8, and -9 in compounds 1 and 2.

Moreover, inhibition of NF-κB translocation in MCF-7 cells treated by compound 1 significantly exhibited the association of extrinsic apoptosis pathway.

Acute toxicity results demonstrated the nontoxic nature of the compounds in mice.

Our results showed significant activity towards MCF-7 cells via either intrinsic or extrinsic mitochondrial pathway and are potential candidate for further in vivo and clinical breast cancer studies.