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

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• 作者：Qingjie Liu ; ^{qingjie.liu@bms.com" class="auth_mail" title="E-mail the corresponding author} ; Douglas G. Batt ; Jonathan S. Lippy ; Neha Surti ; Andrew J. Tebben ; Jodi K. Muckelbauer ; Lin Chen ; Yongmi An ; Chiehying Chang ; Matt Pokross ; Zheng Yang ; Haiqing Wang ; James R. Burke ; Percy H. Carter ; Joseph A. Tino
• 关键词：Bruton&rsquo ; s tyrosine kinase (BTK) ; Janus kinase 2 (JAK2) ; Carbazole
• 刊名：Bioorganic & Medicinal Chemistry Letters
• 出版年：2015
• 出版时间：1 October 2015
• 年：2015
• 卷：25
• 期：19
• 页码：4265-4269
• 全文大小：960 K

文摘

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).