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A novel series of 2-methyl-3-phenylquinazolin-4-one derivatives were synthesized and biologically evaluated for their cytotoxic potential against MCF-7, HepG2, and PC-3 cancer cells. Most of the tested compounds showed reasonable safety in the normal human skin melanocyte HFB4 cell line. Compound  4  showed potent cytotoxicity on Hep-G2 cell lines, while compound  9  showed potent cytotoxicity on the MCF-7 cell line, whereas compounds  10  and  12  showed potent cytotoxicity on Hep-G2 cell lines using 5-fluorouracil as a reference standard. Cell division analysis on the tested cell lines revealed that compounds  4 ,  9 ,  10 , and  12  have potent antiproliferative properties. An  in vitro  enzymatic inhibition assay against EGFR-TK confirmed that those compounds have potent EGFR inhibitory activity. The target compounds arrested the cell cycle at the pre-G1 and G2/M phases. Molecular docking simulations showed that all the target compounds possess a common binding pattern like that of Erlotinib.

Design, synthesis, biological evaluation, and molecular docking of novel quinazolinone EGFR inhibitors as targeted anticancer agents