Details

Autor(en) / Beteiligte

• Waelchli, Rudolf
• Bollbuck, Birgit
• Bruns, Christian
• Buhl, Thomas
• Eder, Jörg
• Feifel, Roland
• Hersperger, Rene
• Janser, Philipp
• Revesz, Laszlo
• Zerwes, Hans-Günter
• Schlapbach, Achim

Titel

Design and preparation of 2-benzamido-pyrimidines as inhibitors of IKK

Ist Teil von

• Bioorganic & medicinal chemistry letters, 2006, Vol.16 (1), p.108-112

Ort / Verlag

Oxford: Elsevier Ltd

Erscheinungsjahr

2006

Link zum Volltext

Quelle

MEDLINE

Beschreibungen/Notizen

• A series of 4-substituted 2-benzamido-pyrimidines has been synthesized and evaluated for their IKK2 inhibitory activities. 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.