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

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

  • Bioorg Med Chem Lett. 2009 Feb 15;19(4):1218-23. doi: 10.1016/j.bmcl.2008.12.075.
Martin Allan 1,  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
Affiliations

Affiliation

  • 1 MethylGene Inc., Department of Medicinal Chemistry, 7220 rue Frederick-Banting, Montreal, Que., Canada H4S 2A1.
PMID: 19131248 DOI: 10.1016/j.bmcl.2008.12.075
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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