Design and preparation of 2-benzamido-pyrimidines as inhibitors of IKK
2005; Elsevier BV; Volume: 16; Issue: 1 Linguagem: Inglês
10.1016/j.bmcl.2005.09.035
ISSN1464-3405
AutoresRudolf Waelchli, Birgit Bollbuck, Christian Bruns, Thomas Buhl, Jörg Eder, Roland Feifel, René Hersperger, Philipp Janser, Láśzló Révész, Hans‐Günter Zerwes, Achim Schlapbach,
Tópico(s)Cytokine Signaling Pathways and Interactions
ResumoThe 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.
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