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

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