31924-81-9Relevant articles and documents
COMPOSITIONS AND METHODS FOR SUBSTITUTED 7-(PIPERAZIN-1-YL)PYRAZOLO[1,5-A]PYRIMIDINE ANALOGS AS INHIBITORS OF KRAS
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, (2021/06/22)
In one aspect, the disclosure relates to compounds useful as inhibitors of mutant KRAS proteins, methods of making the same, pharmaceutical compositions comprising the same, and methods of treating cancers associated with mutated forms of KRAS using the same. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present disclosure.
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.
, 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.
Synthesis and biological evaluation of 7-trifluoromethylpyrazolo[1,5-a]pyrimidines as anti-inflammatory and antimicrobial agents
Aggarwal, Ranjana,Masan, Eakta,Kaushik, Pawan,Kaushik, Dhirender,Sharma, Chetan,Aneja
, p. 16 - 24 (2015/03/05)
A series of 2-H/methyl-3-phenyl-5-alkyl/aryl/heteroaryl-7-trifluoromethylpyrazolo[1,5-a]pyrimidines (4a-l) were synthesized by refluxing 3(5)-amino-4-phenyl-5(3)-H/methyl-1H-pyrazoles (1-2) with trifluoromethyl-?2-diketones (3a-f) in ethanol for 6 h. The