Waelchli Rudolf, Bollbuck Birgit, Bruns Christian, Buhl Thomas, Eder Jörg, Feifel Roland, Hersperger Rene, Janser Philipp, Revesz Laszlo, Zerwes Hans-Günter, Schlapbach Achim
Novartis Institutes for BioMedical Research, CH-4002 Basel, Switzerland.
Bioorg Med Chem Lett. 2006 Jan 1;16(1):108-12. doi: 10.1016/j.bmcl.2005.09.035. Epub 2005 Oct 19.
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 IC(50) values of 40 and 25 nM, respectively. Compound 16 also demonstrated significant in vivo activity in an acute model of cytokine release.
描述了作为新型IKK抑制剂的2-苯甲酰胺基嘧啶的设计、合成及生物学评价。通过对先导化合物3进行优化，确定化合物16和24为IKK2的良好抑制剂，其IC(50)值分别为40 nM和25 nM。化合物16在细胞因子释放急性模型中也表现出显著的体内活性。
