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N-Benzyl-1-heteroaryl-3-(trifluoromethyl)-1H-pyrazole-5-carboxamides as inhibitors of co-activator associated arginine methyltransferase 1 (CARM1) |
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| Authors: | Martin Allan Sukhdev Manku Eric Therrien Natalie Nguyen Sylvia Styhler Marie-France Robert Anne-Christine Goulet Andrea J Petschner Gabi Rahil A Robert MacLeod Robert Déziel Jeffrey M Besterman Hannah Nguyen Amal Wahhab |
| Institution: | 1. MethylGene Inc., Department of Medicinal Chemistry, 7220 rue Frederick-Banting, Montreal, Que., Canada H4S 2A1;2. MethylGene Inc., Department of Lead Discovery, 7220 rue Frederick-Banting, Montreal, Que., Canada H4S 2A1;3. MethylGene Inc., Department of Pharmacology and Cell Biology, 7220 rue Frederick-Banting, Montreal, Que., Canada H4S 2A1 |
| 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. |
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