Abstract
A new series of quinazoline-4-one/chalcone hybrids, 7–26, was synthesized in this study as EGFR inhibitors with antiproliferative activity. Target compounds were synthesized and in vitro tested against different cancer cell lines, EGFR, and BRAF enzymes. Three compounds showed the greatest antiproliferative activity and were the most potent EGFR inhibitors. Also, these three compounds improved the level of active caspase-3, 8, and 9 with potent induction of cytochrome c and Bax levels, as well as down regulation of Bcl-2 levels. Finally, the most active inhibitors docked well inside EGFR active sites.
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