4.5 Article

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

期刊

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 19, 期 4, 页码 1218-1223

出版社

PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2008.12.075

关键词

CARM1; Co-activator associated arginine methyltransferase 1; Protein arginine methyltransferases; CARM1 inhibitors

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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. (C) 2008 Elsevier Ltd. All rights reserved.

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