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

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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 the 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.

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

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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, Advance Article
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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. Contreras, C. Morice, A. Barge, A. Ducime, D. Boschi, S. Al-Karadaghi and M. L. Lolli, Med. Chem. Commun., 2018, Advance Article , DOI: 10.1039/C8MD00068A

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