9H-Carbazole-1-carboxamides as potent and selective JAK2 inhibitors

被引：13

作者：

Zimmermann, Kurt ^{[1
]}

Sang, Xiaopeng ^{[1
]}

Mastalerz, Harold A. ^{[1
]}

Johnson, Walter L. ^{[1
]}

Zhang, Guifen ^{[1
]}

Liu, Qingjie ^{[2
]}

Batt, Douglas ^{[2
]}

Lombardo, Louis J. ^{[2
]}

Vyas, Dinesh ^{[1
]}

Trainor, George L. ^{[2
]}

Tokarski, John S. ^{[2
]}

Lorenzi, Matthew V. ^{[2
]}

You, Dan ^{[2
]}

Gottardis, Marco M. ^{[2
]}

Lippy, Jonathan ^{[2
]}

Khan, Javed ^{[2
]}

Sack, John S. ^{[2
]}

Purandare, Ashok V. ^{[2
]}

机构：

[1] Bristol Myers Squibb Co, Wallingford, CT 06492 USA

[2] Bristol Myers Squibb Co, Princeton, NJ 08540 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2015年 / 25卷 / 14期

关键词：

JAK2; JAK; JAK family selectivity; JAK1; JAK3; TYK2; Myeloproliferative disorders; Myeloproliferative neoplasms; DISCOVERY; PATHWAY;

D O I：

10.1016/j.bmcl.2015.04.101

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The discovery, synthesis, and characterization of 9H-carbazole-1-carboxamides as potent and selective ATP-competitive inhibitors of Janus kinase 2 (JAK2) are discussed. Optimization for JAK family selectivity led to compounds 14 and 21, with greater than 45-fold selectivity for JAK2 over all other members of the JAK kinase family. (C) 2015 Elsevier Ltd. All rights reserved.

引用

收藏

页码：2809 / 2812

页数：4

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