title: Synthesis and in vitro evaluation of N-aryl pyrido-quinazolines derivatives as potent epidermal growth factor receptor inhibitors.
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.
authors.forename: Vinay K
authors.initials: VK
authors.lastname: Singh
authors.forename: Himanshu
authors.initials: H
authors.lastname: Sharma
authors.forename: Sanjay K
authors.initials: SK
authors.lastname: Singh
authors.forename: Lakshmi
authors.initials: L
authors.lastname: Gangwar
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000493:pharmacokinetics; D066246:ErbB Receptors / Q000037:antagonists & inhibitors* / Q000378:metabolism; D006207:Half-Life; D054879:Halogenation; D006367:HeLa Cells; D006801:Humans; D009682:Magnetic Resonance Spectroscopy; D051379:Mice; D011799:Quinazolines / Q000138:chemical synthesis / Q000737:chemistry* / Q000493:pharmacokinetics; D014018:Tissue Distribution
chemical_list: D000970:Antineoplastic Agents; D011799:Quinazolines; D066246:ErbB Receptors