4.4 Article

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

Journal

CHEMICAL BIOLOGY & DRUG DESIGN
Volume 82, Issue 1, Pages 119-124

Publisher

WILEY
DOI: 10.1111/cbdd.12133

Keywords

anticancerous; epidermal growth factor receptor; HeLa; quinazolines; spectroscopy

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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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