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

Authors


Corresponding author: Vinay K. Singh, vinayk2003@rediffmail.com

Abstract

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.

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