Discovery of 4-azaindoles as novel inhibitors of c-Met kinase

The SAR and X-ray crystal structure of a series of 4-azaindole inhibitors of c-Met kinase is reported. A series of 4-azaindole inhibitors of c-Met kinase is described. The postulated binding mode was confirmed by an X-ray crystal structure and series optimisation was performed on the basis of this s...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2009-05, Vol.19 (10), p.2780-2784
Hauptverfasser:	Porter, John, Lumb, Simon, Franklin, Richard J., Gascon-Simorte, Jose M., Calmiano, Mark, Riche, Kelly Le, Lallemand, Bénédicte, Keyaerts, Jean, Edwards, Helen, Maloney, Alison, Delgado, Jean, King, Lloyd, Foley, Anne, Lecomte, Fabien, Reuberson, James, Meier, Christoph, Batchelor, Mark
Format:	Artikel
Sprache:	eng
Schlagworte:	Antineoplastic agents Azaindole Biological and medical sciences c-Met Kinase inhibitor Cell Line, Tumor Computer Simulation Crystallography, X-Ray Drug Discovery General aspects Hepatocyte growth factor receptor inhibitor Humans Indoles - chemical synthesis Indoles - chemistry Indoles - pharmacology Kinase inhibitor Medical sciences Pharmacology. Drug treatments Protein Kinase Inhibitors - chemical synthesis Protein Kinase Inhibitors - chemistry Protein Kinase Inhibitors - pharmacology Proto-Oncogene Proteins c-met - antagonists & inhibitors Proto-Oncogene Proteins c-met - metabolism Structure-Activity Relationship
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Beschreibung
Zusammenfassung:	The SAR and X-ray crystal structure of a series of 4-azaindole inhibitors of c-Met kinase is reported. A series of 4-azaindole inhibitors of c-Met kinase is described. The postulated binding mode was confirmed by an X-ray crystal structure and series optimisation was performed on the basis of this structure. Future directions for series development are discussed.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2009.03.110