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

Laurent F A Hennequin; 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

doi:10.1016/j.bmcl.2006.02.025

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. Epub 2006 Mar 3.

Authors

Laurent F A Hennequin¹, 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

Affiliation

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.

MeSH terms

Administration, Oral
Animals
Dogs
ErbB Receptors / antagonists & inhibitors*
Quinazolines / chemical synthesis
Quinazolines / chemistry*
Quinazolines / pharmacokinetics
Quinazolines / pharmacology*
Rats
Structure-Activity Relationship

Substances

Quinazolines
ErbB Receptors