Optimization of pyrazole inhibitors of Coactivator Associated Arginine Methyltransferase 1 (CARM1)

被引：68

作者：

Huynh, Tram ^{[1
]}

Chen, Zhong ^{[1
]}

Pang, Suhong ^{[1
]}

Geng, Jieping ^{[1
]}

Bandiera, Tiziano ^{[2
]}

Bindi, Simona ^{[2
]}

Vianello, Paola ^{[2
]}

Roletto, Fulvia ^{[2
]}

Thieffine, Sandrine ^{[2
]}

Galvani, Arturo ^{[2
]}

Vaccaro, Wayne ^{[1
]}

Poss, Michael A. ^{[1
]}

Trainor, George L. ^{[1
]}

Lorenzi, Matthew V. ^{[1
]}

Gottardis, Marco ^{[1
]}

Jayaraman, Lata ^{[1
]}

Purandare, Ashok V. ^{[1
]}

机构：

[1] Bristol Myers Squibb Pharmaceut Res & Dev, Princeton, NJ 08543 USA

[2] Nerviano Med Sci Oncol Business Unit, I-20014 Milan, Italy

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2009年 / 19卷 / 11期

关键词：

Coactivator associated arginine methyltransferase 1; CARM1; PRMT4; Pyrazole; Methyltransferase; PROTEIN; METHYLATION; TRANSCRIPTION; CORE;

D O I：

10.1016/j.bmcl.2009.04.075

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Design, synthesis, and SAR development led to the identification of the potent, novel, and selective pyrazole based inhibitor (7f) of Coactivator Associated Arginine Methyltransferase (CARM1). (C) 2009 Elsevier Ltd. All rights reserved.

引用

页码：2924 / 2927

页数：4

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