38377-59-2Relevant academic research and scientific papers
Copper-catalysed: N -arylation of 5-aminopyrazoles: A simple route to pyrazolo[3,4- b] indoles
Chatterjee, Arpita,Murmu, Chudamani,Peruncheralathan, S.
supporting information, p. 6571 - 6581 (2020/11/07)
A copper-catalysed intramolecular N-arylation of 5-aminopyrazoles is demonstrated for the first time. Highly substituted pyrazolo[3,4-b]indoles are synthesized. In particular, the indole core is decorated with halogens and alkyl and methoxy groups. Furthermore, a selective N-arylation of unsymmetrical diaryl bromide containing pyrazoles is exemplified, resulting in valuable pyrazolo[1,5-a]benzimidazoles. This journal is
N -Acetyl-3-aminopyrazoles block the non-canonical NF-kB cascade by selectively inhibiting NIK
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.
supporting information, p. 963 - 968 (2018/06/27)
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.
