Synthesis and In Vitro Evaluation of N‐Aryl Pyrido‐Quinazolines Derivatives as Potent Epidermal Growth Factor Receptor Inhibitors

A series of pyrido‐quinazolines have been synthesised, characterized, and tested for their in vitro epidermal growth factor receptor (EGFR) tyrosine kinase inhibitory activity. The compounds were prepared from Alkylideno/arylideno‐bis‐ureas. Their final structure of the compounds was elucidated on the basis of spectral studies (IR, 1H NMR, FT‐IR, and EI‐MS). The cellular EGFR internalization response of selected compounds was evaluated using HeLa cells. Most of the synthesized compounds displayed potent EGFR‐TK inhibitory activity and structurally halogenated derivatives had a pronounced effect in inhibiting EGFR internalization.