Inhibitors of epidermal growth factor receptor tyrosine kinase: optimisation of potency and in vivo pharmacokinetics

  • Bioorg Med Chem Lett. 2006 Sep 15;16(18):4908-12. doi: 10.1016/j.bmcl.2006.06.054.
Peter Ballard  1 ,  Robert H Bradbury ,  Craig S Harris ,  Laurent F A Hennequin ,  Mark Hickinson ,  Jason G Kettle ,  Jane Kendrew ,  Teresa Klinowska ,  Donald J Ogilvie ,  Stuart E Pearson ,  Emma J Williams ,  Ingrid Wilson
Affiliations
  • 1. AstraZeneca, Mereside, Alderley Park, Macclesfield, Cheshire SK10 4TG, UK.
PMID: 16806916 DOI: 10.1016/j.bmcl.2006.06.054
Abstract

The structure-activity and structure-property relationships of anilinoquinazoline inhibitors of EGFR were investigated. Strategies to lower volume of distribution and shorten half-life through structure and PKA modulation are discussed.