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Synthesis and In Vitro Evaluation of N ‐Aryl Pyrido‐Quinazolines Derivatives as Potent Epidermal Growth Factor Receptor Inhibitors
Author(s) -
Singh Vinay K.,
Sharma Himanshu,
Singh Sanjay K.,
Gangwar Lakshmi
Publication year - 2013
Publication title -
chemical biology and drug design
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.59
H-Index - 77
eISSN - 1747-0285
pISSN - 1747-0277
DOI - 10.1111/cbdd.12133
Subject(s) - internalization , in vitro , chemistry , hela , epidermal growth factor receptor , tyrosine kinase , epidermal growth factor , stereochemistry , biological activity , aryl , biochemistry , receptor , organic chemistry , alkyl
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.