The discovery of 2,5-isomers of triazole-pyrrolopyrimidine as selective Janus kinase 2 (JAK2) inhibitors versus JAK1 and JAK3
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- 作者：Sun-Mi Leea ; Kyoung Bin Yoonb ; Hyo Jeong Leeb ; Jiwon Kimc ; You Kyoung Chungd ; Won-Jea Choe ; Chisato Mukaif ; Sun Choid ; Keon Wook Kangc ; Sun-Young Hanb ; syhan@gnu.ac.kr" class="auth_mail" title="E-mail the corresponding author ; Hyojin Kog ; kohyojin@gist.ac.kr" class="auth_mail" title="E-mail the corresponding author ; Yong-Chul Kima ; g ; yongchul@gist.ac.kr" class="auth_mail" title="E-mail the corresponding author
- 关键词：JAK2 ; JAK2V617F ; JAK2 inhibitor ; STAT (signal transducer and activator of transcription) ; 4-(2 ; 5-Triazole)-pyrrolopyrimidine
- 刊名：Bioorganic & Medicinal Chemistry
- 出版年：2016
- 出版时间：1 November 2016
- 年：2016
- 卷：24
- 期：21
- 页码：5036-5046
- 全文大小：847 K
文摘
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We discovered a potent and selective inhibitor of JAK2, compared to JAK1 and -3.
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2,5-Triazole regioisomers showed a tendency to inhibited JAK2 kinase activity.
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54 exhibited 41.9 nM of IC50, and fold selectivity (JAK1/2 10.6, JAK3/2 58.1).