title: Design, synthesis, and biological evaluation of pyridoquinazoline derivatives as potent epidermal growth factor receptor inhibitors.
abstract: Pyridoquinazolines have been synthesized, 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 structures were elucidated on the basis of elemental analyses and spectral studies (infrared, nuclear magnetic resonance [1H NMR], fourier transform infrared spectroscopy [FTIR], and electron ionization mass spectrometry [EI-MS]). Three of the new compounds had IC50 values in the range of 4.5-11.0 nM. The cellular EGFR internalization response of selected compounds was evaluated using HeLa cells. Three halogenated derivatives had a pronounced effect in inhibiting EGFR internalization.
authors: Department of Applied Sciences, Gold Field Institute of Technology & Management, Faridabad, India.
authors: Sarika
authors: S
authors: Rani
authors: Lata
authors: L
authors: Sridhar
authors: Rakesh
authors: R
authors: Srivastava
authors: Vinay K
authors: VK
authors: Singh
mesh_terms: D000818:Animals; D066246:ErbB Receptors / Q000037:antagonists & inhibitors* / Q000378:metabolism; D005260:Female; D006367:HeLa Cells; D006801:Humans; D008279:Magnetic Resonance Imaging; D051379:Mice; D008807:Mice, Inbred BALB C; D047428:Protein Kinase Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology*; D011725:Pyridines / Q000138:chemical synthesis* / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology*; D011799:Quinazolines / Q000138:chemical synthesis* / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology*; D011817:Rabbits; D013329:Structure-Activity Relationship
chemical_list: D047428:Protein Kinase Inhibitors; D011725:Pyridines; D011799:Quinazolines; D066246:ErbB Receptors