1.
Bioorg Med Chem Lett
; 19(10): 2780-4, 2009 May 15.
Article
in English
| MEDLINE
| ID: mdl-19369077
ABSTRACT
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.
Subject(s)
Indoles/chemistry , Protein Kinase Inhibitors/chemistry , Proto-Oncogene Proteins c-met/antagonists & inhibitors , Cell Line, Tumor , Computer Simulation , Crystallography, X-Ray , Drug Discovery , Humans , Indoles/chemical synthesis , Indoles/pharmacology , Protein Kinase Inhibitors/chemical synthesis , Protein Kinase Inhibitors/pharmacology , Proto-Oncogene Proteins c-met/metabolism , Structure-Activity Relationship
2.
Bioorg Med Chem Lett
; 19(2): 397-400, 2009 Jan 15.
Article
in English
| MEDLINE
| ID: mdl-19059779
ABSTRACT
A series of quinoxaline inhibitors of c-Met kinase is described. The postulated binding mode was confirmed by an X-ray crystal structure and optimisation of the series was performed on the basis of this structure. Future directions for development of the series are discussed together with the identification of a novel quinoline scaffold.
