(1H-imidazo[4,5-c]pyridin-2-yl)-1,2,5-oxadiazol-3-ylamine derivatives: further optimisation as highly potent and selective MSK-1-inhibitors.
The novel imidazo[4,5-c]pyridine 1,2,5-oxadiazol-3-yl template affords an excellent start point for identification of inhibitors of a number of protein kinases. Here we report on its optimisation for mitogen and stress-activated protein kinase-1 (MSK-1) inhibitory activity, and selectivity over other kinases.
Bamford
Mark J
MJ
GlaxoSmithKline Pharmaceuticals, Neurology & GI Centre of Excellence for Drug Discovery, New Frontiers Science Park, Third Avenue, Harlow, Essex CM19 5AW, UK. Mark_J_Bamford@GSK.com
Bailey
Nicholas
N
Davies
Susannah
S
Dean
David K
DK
Francis
Leann
L
Panchal
Terence A
TA
Parr
Christopher A
CA
Sehmi
Sanjeet
S
Steadman
Jon G
JG
Takle
Andrew K
AK
Townsend
James T
JT
Wilson
David M
DM
D000588:Amines / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D004791:Enzyme Inhibitors / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D007093:Imidazoles / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D015394:Molecular Structure; D010069:Oxadiazoles / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D011725:Pyridines / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D038744:Ribosomal Protein S6 Kinases, 90-kDa / Q000037:antagonists & inhibitors*; D013329:Structure-Activity Relationship
D000588:Amines; D004791:Enzyme Inhibitors; D007093:Imidazoles; D010069:Oxadiazoles; D011725:Pyridines; D038744:Ribosomal Protein S6 Kinases, 90-kDa; C116919:mitogen and stress-activated protein kinase 1