Novel 4-anilinoquinazolines with C-6 carbon-linked side chains: synthesis and structure-activity relationship of a series of potent, orally active, EGF receptor tyrosine kinase inhibitors

  • Bioorg Med Chem Lett. 2006 May 15;16(10):2672-6. doi: 10.1016/j.bmcl.2006.02.025.
Laurent F A Hennequin  1 ,  Peter Ballard ,  F Tom Boyle ,  Bénédicte Delouvrié ,  Rebecca P A Ellston ,  Chris T Halsall ,  Craig S Harris ,  Kevin Hudson ,  Jane Kendrew ,  J Elizabeth Pease ,  Helen S Ross ,  Peter Smith ,  Jennifer L Vincent
Affiliations
  • 1. AstraZeneca, Centre de Recherches, Z.I. La Pompelle, B.P. 1050, Chemin de Vrilly, 51689 Reims, Cedex 2, France. [email protected]
PMID: 16516473 DOI: 10.1016/j.bmcl.2006.02.025
Abstract

The structure-activity relationship of a novel subseries of 4-anilinoquinazoline EGFR inhibitors substituted at the C-6 position with carbon-linked side chains has been investigated. This exploration has led to the discovery of novel aminomethyl carboxamides with good biological, pharmacokinetic and physical properties.