title: Inhibitors of epidermal growth factor receptor tyrosine kinase: Novel C-5 substituted anilinoquinazolines designed to target the ribose pocket.
abstract: A series of novel C-5 substituted anilinoquinazolines, selected on the basis of docking experiments and overlays with ATP in the active site of EGFR tyrosine kinase, have been prepared and found to be potent inhibitors. In vivo pharmacokinetics and disease model activity are discussed.
authors.affiliation: AstraZeneca, Mereside, Alderley Park, Macclesfield, Cheshire SK10 4TG, UK.
authors.forename: Peter
authors.initials: P
authors.lastname: Ballard
authors.forename: Robert H
authors.initials: RH
authors.lastname: Bradbury
authors.forename: Craig S
authors.initials: CS
authors.lastname: Harris
authors.forename: Laurent F A
authors.initials: LF
authors.lastname: Hennequin
authors.forename: Mark
authors.initials: M
authors.lastname: Hickinson
authors.forename: Paul D
authors.initials: PD
authors.lastname: Johnson
authors.forename: Jason G
authors.initials: JG
authors.lastname: Kettle
authors.forename: Teresa
authors.initials: T
authors.lastname: Klinowska
authors.forename: Andrew G
authors.initials: AG
authors.lastname: Leach
authors.forename: Remy
authors.initials: R
authors.lastname: Morgentin
authors.forename: Martin
authors.initials: M
authors.lastname: Pass
authors.forename: Donald J
authors.initials: DJ
authors.lastname: Ogilvie
authors.forename: Annie
authors.initials: A
authors.lastname: Olivier
authors.forename: Nicolas
authors.initials: N
authors.lastname: Warin
authors.forename: Emma J
authors.initials: EJ
authors.lastname: Williams
mesh_terms: D000255:Adenosine Triphosphate / Q000378:metabolism; D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000493:pharmacokinetics / Q000494:pharmacology; D001665:Binding Sites; D049109:Cell Proliferation / Q000187:drug effects; D003110:Colonic Neoplasms / Q000188:drug therapy; D066246:ErbB Receptors / Q000037:antagonists & inhibitors*; D005260:Female; D006801:Humans; D007624:KB Cells / Q000187:drug effects; D051379:Mice; D008819:Mice, Nude; D015394:Molecular Structure; D047428:Protein Kinase Inhibitors / Q000138:chemical synthesis / Q000493:pharmacokinetics / Q000494:pharmacology; D011799:Quinazolines / Q000138:chemical synthesis / Q000493:pharmacokinetics / Q000494:pharmacology; D051381:Rats; D012266:Ribose / Q000378:metabolism*; D013329:Structure-Activity Relationship; D014183:Transplantation, Heterologous; D014407:Tumor Cells, Cultured
chemical_list: D000970:Antineoplastic Agents; D047428:Protein Kinase Inhibitors; D011799:Quinazolines; D012266:Ribose; D000255:Adenosine Triphosphate; D066246:ErbB Receptors