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

被引：71

作者：

Allan, Martin ^{[1
]}

Manku, Sukhdev ^{[1
]}

Therrien, Eric ^{[1
]}

Nguyen, Natalie ^{[1
]}

Styhler, Sylvia ^{[3
]}

Robert, Marie-France ^{[3
]}

Goulet, Anne-Christine ^{[3
]}

Petschner, Andrea J. ^{[2
]}

Rahil, Gabi ^{[2
]}

MacLeod, A. Robert ^{[3
]}

Deziel, Robert ^{[1
]}

Besterman, Jeffrey M. ^{[3
]}

Nguyen, Hannah ^{[3
]}

Wahhab, Amal ^{[1
]}

机构：

[1] MethylGene Inc, Dept Med Chem, Montreal, PQ H4S 2A1, Canada

[2] MethylGene Inc, Dept Lead Discovery, Montreal, PQ H4S 2A1, Canada

[3] MethylGene Inc, Dept Pharmacol & Cell Biol, Montreal, PQ H4S 2A1, Canada

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2009年 / 19卷 / 04期

关键词：

CARM1; Co-activator associated arginine methyltransferase 1; Protein arginine methyltransferases; inhibitors; GENE-EXPRESSION; HISTONE/PROTEIN METHYLTRANSFERASE; TRANSCRIPTIONAL COACTIVATOR; PROTEIN METHYLTRANSFERASE; ANDROGEN RECEPTOR; STABLY EXPRESSES; CELL-LINE; METHYLATION; RNA; ACETYLTRANSFERASE;

D O I：

10.1016/j.bmcl.2008.12.075

中图分类号：

R914 [药物化学];

学科分类号：

100705 [微生物与生化药学];

摘要：

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.

引用

页码：1218 / 1223

页数：6

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