9H-咔唑-1-甲酰胺作为强效且选择性的JAK2抑制剂。
9H-Carbazole-1-carboxamides as potent and selective JAK2 inhibitors.
作者信息
Zimmermann Kurt, Sang Xiaopeng, Mastalerz Harold A, Johnson Walter L, Zhang Guifen, Liu Qingjie, Batt Douglas, Lombardo Louis J, Vyas Dinesh, Trainor George L, Tokarski John S, Lorenzi Matthew V, You Dan, Gottardis Marco M, Lippy Jonathan, Khan Javed, Sack John S, Purandare Ashok V
机构信息
Bristol-Myers Squibb Co., 5 Research Parkway, Wallingford, CT 06492-1951, USA.
Bristol-Myers Squibb Co., 5 Research Parkway, Wallingford, CT 06492-1951, USA.
出版信息
Bioorg Med Chem Lett. 2015 Jul 15;25(14):2809-12. doi: 10.1016/j.bmcl.2015.04.101. Epub 2015 May 11.
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.
本文讨论了9H-咔唑-1-甲酰胺作为强效且选择性的Janus激酶2（JAK2）的ATP竞争性抑制剂的发现、合成及表征。对JAK家族选择性的优化得到了化合物14和21，其对JAK2的选择性比对JAK激酶家族的所有其他成员高45倍以上。
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