1.
Bioorg Med Chem Lett
; 15(14): 3402-6, 2005 Jul 15.
Article
in English
| MEDLINE
| ID: mdl-15950465
ABSTRACT
A novel series of imidazo[4,5-c]pyridines bearing a 1,2,5-oxadiazol-3-ylamine functionality has been developed. These are potent inhibitors of mitogen and stress-activated protein kinase-1.
Subject(s)
Amines/pharmacology , Enzyme Inhibitors/pharmacology , Imidazoles/pharmacology , Oxadiazoles/pharmacology , Pyridines/pharmacology , Ribosomal Protein S6 Kinases, 90-kDa/antagonists & inhibitors , Amines/chemical synthesis , Amines/classification , Enzyme Inhibitors/chemical synthesis , Enzyme Inhibitors/classification , Imidazoles/chemical synthesis , Imidazoles/classification , Molecular Structure , Oxadiazoles/chemical synthesis , Oxadiazoles/classification , Pyridines/chemical synthesis , Pyridines/classification , Structure-Activity Relationship
2.
Bioorg Med Chem Lett
; 15(14): 3407-11, 2005 Jul 15.
Article
in English
| MEDLINE
| ID: mdl-15955699
ABSTRACT
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.