Structure activity relationships of quinoline-containing c-Met inhibitors.
A series of quinoline-containing c-Met inhibitors were prepared and studied. Chemistry was developed to introduce a pyridyl moiety onto the 2-aryl ring present in a lead molecule which mitigated the potential for quinone formation relative to the original compound. The study also assessed the importance of an acylthiourea moiety present in the lead structure for effective binding to the c-Met protein ATP site.
Kung
Pei-Pei
PP
Pfizer Global Research and Development, La Jolla Laboratories, 10770 Science Center Drive, San Diego, CA 92121, USA. peipeikung@pfizer.com
Funk
Lee
L
Meng
Jerry
J
Alton
Gordon
G
Padrique
Ellen
E
Mroczkowski
Barbara
B
D009682:Magnetic Resonance Spectroscopy; D013058:Mass Spectrometry; D047428:Protein Kinase Inhibitors / Q000737:chemistry* / Q000494:pharmacology*; D019859:Proto-Oncogene Proteins c-met / Q000037:antagonists & inhibitors*; D011804:Quinolines / Q000494:pharmacology*; D013329:Structure-Activity Relationship
D047428:Protein Kinase Inhibitors; D011804:Quinolines; C037219:quinoline; D019859:Proto-Oncogene Proteins c-met