2. Academic Validation
  3. Inhibitors of epidermal growth factor receptor tyrosine kinase: optimisation of potency and in vivo pharmacokinetics

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

Affiliation

  • 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.

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