N -Acetyl-3-aminopyrazoles block the non-canonical NF-kB cascade by selectively inhibiting NIK
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.
Pippione, Agnese C.,Sainas, Stefano,Federico, Antonella,Lupino, Elisa,Piccinini, Marco,Kubbutat, Michael,Contreras, Jean-Marie,Morice, Christophe,Barge, Alessandro,Ducime, Alex,Boschi, Donatella,Al-Karadaghi, Salam,Lolli, Marco L.
p. 963 - 968
(2018/06/27)
Structure and tautomerism of 4-substituted 3(5)-aminopyrazoles in solution and in the solid state: NMR study and Ab initio calculations
Annular tautomerism of 3(5)-aminopyrazoles containing a cyano, thiocyanato, or aryl substituent in the 4-position has been studied by 1H and 13C NMR in solution, cross-polarization and magic-angle spinning 13C NMR in the s
Emelina,Petrov,Filyukov
p. 412 - 421
(2014/06/09)
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