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N-Acetyl-3-aminopyrazoles block the non canonical NF-kB cascade by selectively inhibiting NIK

Abstract

NF-κB-inducing kinase (NIK), an oncogenic drug target that is associated with various cancers, is a central signalling component of the non-canonical pathway. A blind screening process, which established that amino pyrazole related scaffolds have an effect on IKKbeta, led to a hit-to-lead optimization process that identified aminopyrazole 3a as a low μM selective NIK inhibitor. Compound 3a effectively inhibited the NIK-dependent activation of the NF-κB pathway in tumour cells, confirming its selective inhibitory profile.

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Publication details

The article was received on 05 Feb 2018, accepted on 07 Apr 2018 and first published on 12 Apr 2018


Article type: Research Article
DOI: 10.1039/C8MD00068A
Citation: Med. Chem. Commun., 2018, Accepted Manuscript
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    N-Acetyl-3-aminopyrazoles block the non canonical NF-kB cascade by selectively inhibiting NIK

    A. C. Pippione, S. Sainas, A. Federico, E. LUPINO, M. Piccinini, M. Kubbutat, J. M. Contreras, C. Morice, A. Barge, A. DUCIME, D. boschi, S. Al-Karadaghi and M. L. L. LOLLI, Med. Chem. Commun., 2018, Accepted Manuscript , DOI: 10.1039/C8MD00068A

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