677326-67-9Relevant academic research and scientific papers
1, 3-diaryl-5-alkoxy pyrazole compound as well as preparation method and application thereof
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Paragraph 0013; 0014; 0015; 0016, (2018/03/26)
The invention discloses a 1, 3-diaryl-5-alkoxy pyrazole compound as well as a preparation method and application thereof. The compound is specifically 1-(4-(2-chloroacetamido)phenyl)-3-(3,4-dichlorophenyl)-5-(2-methoxyethoxy)pyrazole, and has a structural
Synthesis and structure–activity relationship studies of MI-2 analogues as MALT1 inhibitors
Wu, Guolin,Wang, Haixia,Zhou, Wenhui,Zeng, Bihua,Mo, Wenhui,Zhu, Kejie,Liu, Rong,Zhou, Jia,Chen, Ceshi,Chen, Haijun
supporting information, p. 3321 - 3344 (2018/05/23)
Recent studies revealed that MALT1 is a promising therapeutic target for the treatment of ABC-DLBCL. Among several reported MALT1 inhibitors, MI-2 as an irreversible inhibitor represents a new class of ABC-DLBCL therapeutics. Due to its inherent potential cross-reactivity, further structure–activity relationship (SAR) study is imperative. In this work, five focused compound libraries based on the chemical structure of MI-2 are designed and synthesized. The systematic SARs revealed that the side chain of 2-methoxyethoxy has little impact on the activity and can be replaced by other functionalized groups, providing new MI-2 analogues with retained or enhanced potency. Compounds 81–83 with terminal hydroxyl group as side chain displayed enhanced activities against MALT1. Replacement of triazole core with pyrazole is also tolerant, while structural modifications on other sites are detrimental. These findings will facilitate further development of small-molecule MALT1 inhibitors.
PhIO/Et3N ? 3HF-Mediated Formation of Fluorinated 2H-Azirines via Domino Fluorination/Azirination Reaction of Enamines
Zhang, Yong,Zhao, Xiaoyuan,Zhuang, Chen,Wang, Senlin,Zhang-Negrerie, Daisy,Du, Yunfei
supporting information, p. 2107 - 2112 (2018/04/19)
A variety of enamine carboxylic esters and enaminones were converted to the biologically interesting fluorinated 2H-azirines through reactions with PhIF2 generated in situ by PhIO and Et3N ? 3HF in 1,2-dichroloethane, which features the hypervalent iodine reagents-mediated introduction of fluorine atom and formation of the 2H-azirine skeleton under metal-free conditions. The domino reaction is postulated to proceed via a PhIF2-mediated oxidative fluorination and a subsequent azirination of the fluorinated enamine intermediates. (Figure presented.).
1,3,5-trisubstituted pyrazole compound as well as preparation method and application thereof
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Paragraph 0012; 0013; 0014; 0015; 0016; 0017; 0018, (2017/10/07)
The invention discloses a 1,3,5-trisubstituted pyrazole compound as well as a preparation method and application thereof. The 1,3,5-trisubstituted pyrazole compound is 5-(3,4-dichlorophenyl)-3-(4-(2-chloroacetylamino) phenoxyl)-1-(2-methoxyethyl)pyrazole,
HETEROCYCLIC COMPOUNDS FOR THE INHIBITION OF PASK
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Page/Page column 21, (2012/11/08)
Disclosed herein are new heterocyclic compounds and compositions and their application as pharmaceuticals for the treatment of disease. Methods of inhibiting PAS Kinase (PASK) activity in a human or animal subject are also provided for the treatment of diseases such as diabetes mellitus.
Preparation and evaluation of trisubstituted pyrimidines as phosphatidylinositol 3-kinase inhibitors. 3-Hydroxyphenol analogues and bioisosteric replacements
Large, Jonathan M.,Torr, Jane E.,Raynaud, Florence I.,Clarke, Paul A.,Hayes, Angela,Stefano, Francesca Di,Urban, Frederique,Shuttleworth, Stephen J.,Saghir, Nahid,Sheldrake, Peter,Workman, Paul,McDonald, Edward
scheme or table, p. 836 - 851 (2011/03/19)
Two classes of trisubstituted pyrimidines related to PI-103 1 have been prepared and their inhibitory activities against phosphatidylinositol 3-kinase (PI3K) p110α were determined. From those with direct 6-aryl substitution compound 11a was the most potent inhibitor with an IC50 value of 62 nM, and showed similar activity against other class 1a PI3K isoforms tested, p110β and p110γ. When a linking chain was introduced, as in the second exemplified class, compound 15f inhibited p110α with IC 50 142 nM, and showed greater selectivity towards p110α. Compounds of both classes showed promising inhibition of cellular proliferation in IGROV-1 ovarian cancer cells. Among compounds designed to replace the 3-phenolic motif with structural isosteres, analogues incorporating a 4-indazolyl group possessed enzyme and cellular activities comparable to the parent phenols.
