Design and preparation of 2-benzamido-pyrimidines as inhibitors of IKK
Design and preparation of 2-benzamido-pyrimidines as inhibitors of IKK
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DOI：
10.1016/j.bmcl.2005.09.035
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发表时间：
2006-01-01
影响因子：
2.7
通讯作者：
Schlapbach, A
中科院分区：
文献类型：
--
作者：
Waelchli, R;Bollbuck, B;Schlapbach, A
介绍了新型IKK抑制剂2-苯并脒的设计、合成和生物学评价。通过对先导化合物3的优化，化合物16和24为IKK2的良好抑制剂，IC50值分别为40和25 nM。化合物16在细胞因子释放急性模型中也显示出显著的体内活性。(c) 2005 Elsevier Ltd版权所有。
The design, synthesis, and the biological evaluation of 2-benzamido-pyrimidines as novel IKK inhibitors are described. By optimization of the lead compound 3, compounds 16 and 24 are identified as good inhibitors of IKK2 with IC50 values of 40 and 25 nM, respectively. Compound 16 also demonstrated significant in vivo activity in an acute model of cytokine release. (c) 2005 Elsevier Ltd. All rights reserved.