2. Academic Validation
  3. 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

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

Affiliation

  • 1 AstraZeneca, Centre de Recherches, Z.I. La Pompelle, B.P. 1050, Chemin de Vrilly, 51689 Reims, Cedex 2, France. Laurent.Hennequin@astrazeneca.com
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.

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