Design and synthesis of carbazole carboxamides as promising inhibitors of Bruton's tyrosine kinase (BTK) and Janus kinase 2 (JAK2)

被引：22

作者：

Liu, Qingjie ^{[1
]}

Batt, Douglas G. ^{[1
]}

Lippy, Jonathan S. ^{[1
]}

Surti, Neha ^{[1
]}

Tebben, Andrew J. ^{[1
]}

Muckelbauer, Jodi K. ^{[1
]}

Chen, Lin ^{[1
]}

An, Yongmi ^{[1
]}

Chang, Chiehying ^{[1
]}

Pokross, Matt ^{[1
]}

Yang, Zheng ^{[1
]}

Wang, Haiqing ^{[1
]}

Burke, James R. ^{[1
]}

Carter, Percy H. ^{[1
]}

Tino, Joseph A. ^{[1
]}

机构：

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

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2015年 / 25卷 / 19期

关键词：

Bruton's tyrosine kinase (BTK); Janus kinase 2 (JAK2); Carbazole; B-CELL; MYELOPROLIFERATIVE DISORDERS; POTENT; DISCOVERY; RITUXIMAB; ARTHRITIS; THERAPY;

D O I：

10.1016/j.bmcl.2015.07.102

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Four series of disubstituted carbazole-1-carboxamides were designed and synthesised as inhibitors of Bruton's tyrosine kinase (BTK). 4,7- and 4,6-disubstituted carbazole-1-carboxamides were potent and selective inhibitors of BTK, while 3,7- and 3,6-disubstituted carbazole-1-carboxamides were potent and selective inhibitors of Janus kinase 2 (JAK2). (C) 2015 Elsevier Ltd. All rights reserved.

引用

页码：4265 / 4269

页数：5

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