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

Waelchli, Rudolf and Bollbuck, Birgit and Bruns, Christian and Buhl, Thomas and Eder, Joerg and Feifel, Roland and Hersperger, Rene and Janser, Philipp and Revesz, Laszlo and Zerwes, Hans-Guenter and Schlapbach, Achim (2006) Design and preparation of 2-benzamido-pyrimidines as inhibitors of IKK. Bioorganic & Medicinal Chemistry Letters, 16 (1). pp. 108-112. ISSN 0960-894X

Abstract

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.

Item Type: Article
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Additional Information: author can archive post-print (ie final draft post-refereeing); Publisher's version/PDF cannot be used
Keywords: 2-Benzamido-pyrimidines; IKK inhibitors; IKK2; In vivo activity
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Date Deposited: 14 Dec 2009 13:59
Last Modified: 31 Jan 2013 01:15
URI: https://oak.novartis.com/id/eprint/490

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