Synthesis and structure-activity relationship of 4-(2-aryl-cyclopropylamino)-quinoline-3-carbonitriles as EGFR tyrosine kinase inhibitors.
Synthesis and structure-activity relationship of a series of 4-(2-aryl-cyclopropylamino)-quinoline-3-carbonitrile derivatives as EGFR inhibitors is described. Compounds 29 and 30 showed potent in vitro inhibitory activity in the enzymatic assay as well as in the functional cellular assay. They are moderately selective against other types of tyrosine kinases.
Pannala
Madhavi
M
Department of Chemistry, Tanabe Research Laboratories USA, Inc., 4540 Towne Centre Court, San Diego, CA 92121, USA.
Kher
Sunil
S
Wilson
Norma
N
Gaudette
John
J
Sircar
Ila
I
Zhang
Shao-Hui
SH
Bakhirev
Alexei
A
Yang
Guang
G
Yuen
Phoebe
P
Gorcsan
Frank
F
Sakurai
Naoki
N
Barbosa
Miguel
M
Cheng
Jie-Fei
JF
D004791:Enzyme Inhibitors / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D066246:ErbB Receptors / Q000037:antagonists & inhibitors*; D009570:Nitriles / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D011804:Quinolines / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D013329:Structure-Activity Relationship