title: N-Benzyl-1-heteroaryl-3-(trifluoromethyl)-1H-pyrazole-5-carboxamides as inhibitors of co-activator associated arginine methyltransferase 1 (CARM1).
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.
authors.affiliation: MethylGene Inc., Department of Medicinal Chemistry, 7220 rue Frederick-Banting, Montreal, Que., Canada H4S 2A1.
authors.forename: Martin
authors.initials: M
authors.lastname: Allan
authors.forename: Sukhdev
authors.initials: S
authors.lastname: Manku
authors.forename: Eric
authors.initials: E
authors.lastname: Therrien
authors.forename: Natalie
authors.initials: N
authors.lastname: Nguyen
authors.forename: Sylvia
authors.initials: S
authors.lastname: Styhler
authors.forename: Marie-France
authors.initials: MF
authors.lastname: Robert
authors.forename: Anne-Christine
authors.initials: AC
authors.lastname: Goulet
authors.forename: Andrea J
authors.initials: AJ
authors.lastname: Petschner
authors.forename: Gabi
authors.initials: G
authors.lastname: Rahil
authors.forename: A
authors.initials: A
authors.lastname: Robert Macleod
authors.forename: Robert
authors.initials: R
authors.lastname: Déziel
authors.forename: Jeffrey M
authors.initials: JM
authors.lastname: Besterman
authors.forename: Hannah
authors.initials: H
authors.lastname: Nguyen
authors.forename: Amal
authors.initials: A
authors.lastname: Wahhab
mesh_terms: 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*
chemical_list: D000577:Amides; D011720:Pyrazoles; D013876:Thiophenes; D011484:Protein-Arginine N-Methyltransferases; C119966:coactivator-associated arginine methyltransferase 1