Abstract
A series of N-benzyl-1-heteroaryl-3-(trifluoromethyl)-1H-pyrazole-5-carboxamides targeting co-activator associated arginine methyltransferase 1 (CARM1) have been designed and synthesized. The potency of these inhibitors was influenced by the nature of the heteroaryl fragment with the thiophene analogues being superior to thiazole, pyridine, isoindoline and benzofuran based inhibitors.
MeSH terms
-
Amides / chemical synthesis*
-
Amides / chemistry
-
Amides / pharmacology*
-
Combinatorial Chemistry Techniques
-
Molecular Structure
-
Protein-Arginine N-Methyltransferases / antagonists & inhibitors*
-
Pyrazoles / chemical synthesis*
-
Pyrazoles / chemistry
-
Pyrazoles / pharmacology*
-
Thiophenes / chemical synthesis*
-
Thiophenes / chemistry
-
Thiophenes / pharmacology*
Substances
-
Amides
-
Pyrazoles
-
Thiophenes
-
Protein-Arginine N-Methyltransferases
-
coactivator-associated arginine methyltransferase 1