Discovery of 4-azaindoles as novel inhibitors of c-Met kinase.
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.
UCB Celltech, Slough, United Kingdom. john.porter@ucb.com
John
J
Porter
Simon
S
Lumb
Richard J
RJ
Franklin
Jose M
JM
Gascon-Simorte
Mark
M
Calmiano
Kelly Le
KL
Riche
Bénédicte
B
Lallemand
Jean
J
Keyaerts
Helen
H
Edwards
Alison
A
Maloney
Jean
J
Delgado
Lloyd
L
King
Anne
A
Foley
Fabien
F
Lecomte
James
J
Reuberson
Christoph
C
Meier
Mark
M
Batchelor
D045744:Cell Line, Tumor; D003198:Computer Simulation; D018360:Crystallography, X-Ray; D055808:Drug Discovery; D006801:Humans; D007211:Indoles / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D047428:Protein Kinase Inhibitors / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D019859:Proto-Oncogene Proteins c-met / Q000037:antagonists & inhibitors* / Q000378:metabolism; D013329:Structure-Activity Relationship
C522780:4-azaindole; D007211:Indoles; D047428:Protein Kinase Inhibitors; D019859:Proto-Oncogene Proteins c-met