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 , 1 H 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.