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 import...

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Bibliographic Details
Published in:European journal of medicinal chemistry 2008-06, Vol.43 (6), p.1321-1329
Main Authors: Kung, Pei-Pei, Funk, Lee, Meng, Jerry, Alton, Gordon, Padrique, Ellen, Mroczkowski, Barbara
Format: Article
Language:English
Subjects:
Antineoplastic agents
Biological and medical sciences
c-Met
General aspects
Magnetic Resonance Spectroscopy
Mass Spectrometry
Medical sciences
Pharmacology. Drug treatments
Protein Kinase Inhibitors - chemistry
Protein Kinase Inhibitors - pharmacology
Proto-Oncogene Proteins c-met - antagonists & inhibitors
Quinoline
Quinolines - pharmacology
Structure-Activity Relationship
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Summary: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. [Display omitted]
ISSN:0223-5234
1768-3254
DOI:10.1016/j.ejmech.2007.08.011