The identification of potent and selective imidazole-based inhibitors of B-Raf kinase.
A novel triarylimidazole derivative, SB-590885 (33), bearing a 2,3-dihydro-1H-inden-1-one oxime substituent has been identified as a potent and extremely selective inhibitor of B-Raf kinase.
Takle
Andrew K
AK
Department of Medicinal Chemistry, Neurology and GI Centre of Excellence for Drug Discovery, GlaxoSmithKline Pharmaceuticals, New Frontiers Science Park, Third Avenue, Harlow, Essex CM19 5AW, UK. Andy.K.Takle@gsk.com
Brown
Murray J B
MJ
Davies
Susannah
S
Dean
David K
DK
Francis
Gerraint
G
Gaiba
Alessandra
A
Hird
Alex W
AW
King
Frank D
FD
Lovell
Peter J
PJ
Naylor
Antoinette
A
Reith
Alastair D
AD
Steadman
Jon G
JG
Wilson
David M
DM
D003500:Cyclization; D007093:Imidazoles / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D015394:Molecular Structure; D048493:Proto-Oncogene Proteins B-raf / Q000037:antagonists & inhibitors* / Q000737:chemistry; D013329:Structure-Activity Relationship
D007093:Imidazoles; C508204:SB-590885; D048493:Proto-Oncogene Proteins B-raf