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  • Title: Inhibitors of epidermal growth factor receptor tyrosine kinase: Novel C-5 substituted anilinoquinazolines designed to target the ribose pocket.
    Author: Ballard P, Bradbury RH, Harris CS, Hennequin LF, Hickinson M, Johnson PD, Kettle JG, Klinowska T, Leach AG, Morgentin R, Pass M, Ogilvie DJ, Olivier A, Warin N, Williams EJ.
    Journal: Bioorg Med Chem Lett; 2006 Mar 15; 16(6):1633-7. PubMed ID: 16380259.
    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.
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