88327-91-7Relevant articles and documents
Optimization of norbornyl-based carbocyclic nucleoside analogs as cyclin-dependent kinase 2 inhibitors
K?prülüo?lu, Cemal,Dejmek, Milan,?ála, Michal,Ajani, Haresh,H?ebabecky, Hubert,Fanfrlík, Jind?ich,Jorda, Radek,Dra?ínsky, Martin,Procházková, Eli?ka,?ácha, Pavel,Kry?tof, Vladimír,Hobza, Pavel,Lep?ík, Martin,Nencka, Radim
, (2020/03/30)
We report on the discovery of norbornyl moiety as a novel structural motif for cyclin-dependent kinase 2 (CDK2) inhibitors which was identified by screening a carbocyclic nucleoside analogue library. Three micromolar hits were expanded by the use of medic
1,2-Benzisothiazol-3-one derivatives as a novel class of small-molecule caspase-3 inhibitors
Wu, Lixin,Lu, Meiqi,Yan, Zhihui,Tang, Xiaobin,Sun, Bo,Liu, Wei,Zhou, Honggang,Yang, Cheng
, p. 2416 - 2426 (2014/05/06)
A novel series of 1,2-benzisothiazol-3-one derivatives was synthesized and their biological activities were evaluated for inhibiting caspase-3 and -7 activities, in which some of them showed low nanomolar potency against caspase-3 in vitro and significant protection against apoptosis in a camptothecin-induced Jurkat T cells system. Among the tested compounds, compound 5i exhibited the most potent caspase-3 inhibitory activity (IC50 = 1.15 nM). The molecular docking predicted the interactions and binding modes of the synthesized inhibitor in the caspase-3 active site.
4,6-DIAMINONICOTINAMIDE COMPOUND
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Page/Page column 41, (2011/09/20)
[Problem] The present invention provides a 4,6-diaminonicotinamide compound which is useful as an active ingredient of a pharmaceutical composition, in particular, a pharmaceutical composition for treating diseases caused by undesirable and/or abnormal cytokine signal transduction. [Means for Solution] The present inventors have extensively studied compounds having a JAK3 inhibitory action, and as a result, they have found that a 4,6-diaminonicotinamide compound which is the compound of the present invention has an excellent JAK3 inhibitory action and is useful as an agent for preventing or treating diseases caused by undesirable and/or abnormal cytokine signal transduction, thereby completing the present invention.