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ID: ALA1136843

Journal: Bioorg Med Chem Lett

Title: N-Benzyl-1-heteroaryl-3-(trifluoromethyl)-1H-pyrazole-5-carboxamides as inhibitors of co-activator associated arginine methyltransferase 1 (CARM1).

Authors: Allan M, Manku S, Therrien E, Nguyen N, Styhler S, Robert MF, Goulet AC, Petschner AJ, Rahil G, Robert Macleod A, Déziel R, Besterman JM, Nguyen H, Wahhab A.

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.

CiteXplore: 19131248

DOI: 10.1016/j.bmcl.2008.12.075