title: Structure activity relationships of quinoline-containing c-Met inhibitors.
abstract: 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.
authors.affiliation: Pfizer Global Research and Development, La Jolla Laboratories, 10770 Science Center Drive, San Diego, CA 92121, USA. peipeikung@pfizer.com
authors.forename: Pei-Pei
authors.initials: PP
authors.lastname: Kung
authors.forename: Lee
authors.initials: L
authors.lastname: Funk
authors.forename: Jerry
authors.initials: J
authors.lastname: Meng
authors.forename: Gordon
authors.initials: G
authors.lastname: Alton
authors.forename: Ellen
authors.initials: E
authors.lastname: Padrique
authors.forename: Barbara
authors.initials: B
authors.lastname: Mroczkowski
mesh_terms: 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
chemical_list: D047428:Protein Kinase Inhibitors; D011804:Quinolines; C037219:quinoline; D019859:Proto-Oncogene Proteins c-met