N-Benzyl-1-heteroaryl-3-(trifluoromethyl)-1H-pyrazole-5-carboxamides as inhibitors of co-activator associated arginine methyltransferase 1 (CARM1).
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.
Allan
Martin
M
MethylGene Inc., Department of Medicinal Chemistry, 7220 rue Frederick-Banting, Montreal, Que., Canada H4S 2A1.
Manku
Sukhdev
S
Therrien
Eric
E
Nguyen
Natalie
N
Styhler
Sylvia
S
Robert
Marie-France
MF
Goulet
Anne-Christine
AC
Petschner
Andrea J
AJ
Rahil
Gabi
G
Robert Macleod
A
A
Déziel
Robert
R
Besterman
Jeffrey M
JM
Nguyen
Hannah
H
Wahhab
Amal
A
D000577:Amides / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D020650:Combinatorial Chemistry Techniques; D015394:Molecular Structure; D011484:Protein-Arginine N-Methyltransferases / Q000037:antagonists & inhibitors*; D011720:Pyrazoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D013876:Thiophenes / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*
D000577:Amides; D011720:Pyrazoles; D013876:Thiophenes; D011484:Protein-Arginine N-Methyltransferases; C119966:coactivator-associated arginine methyltransferase 1