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.
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.
Hennequin
Laurent F A
LF
AstraZeneca, Centre de Recherches, Z.I. La Pompelle, B.P. 1050, Chemin de Vrilly, 51689 Reims, Cedex 2, France. Laurent.Hennequin@astrazeneca.com
Ballard
Peter
P
Boyle
F Tom
FT
Delouvrié
Bénédicte
B
Ellston
Rebecca P A
RP
Halsall
Chris T
CT
Harris
Craig S
CS
Hudson
Kevin
K
Kendrew
Jane
J
Pease
J Elizabeth
JE
Ross
Helen S
HS
Smith
Peter
P
Vincent
Jennifer L
JL
D000284:Administration, Oral; D000818:Animals; D004285:Dogs; D066246:ErbB Receptors / Q000037:antagonists & inhibitors*; D011799:Quinazolines / Q000138:chemical synthesis / Q000737:chemistry* / Q000493:pharmacokinetics / Q000494:pharmacology*; D051381:Rats; D013329:Structure-Activity Relationship
D011799:Quinazolines; D066246:ErbB Receptors