24372-49-4Relevant articles and documents
Betti reaction enables efficient synthesis of 8-hydroxyquinoline inhibitors of 2-oxoglutarate oxygenases
Thinnes,Tumber,Yapp,Scozzafava,Yeh,Chan,Tran,Hsu,Tarhonskaya,Walport,Wilkins,Martinez,Müller,Pugh,Ratcliffe,Brennan,Kawamura,Schofield
supporting information, p. 15458 - 15461 (2015/10/20)
There is interest in developing potent, selective, and cell-permeable inhibitors of human ferrous iron and 2-oxoglutarate (2OG) oxygenases for use in functional and target validation studies. The 3-component Betti reaction enables efficient one-step C-7 functionalisation of modified 8-hydroxyquinolines (8HQs) to produce cell-active inhibitors of KDM4 histone demethylases and other 2OG oxygenases; the work exemplifies how a template-based metallo-enzyme inhibitor approach can be used to give biologically active compounds.
BCRP/ABCG2 INHIBITOR
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Page/Page column 13, (2008/06/13)
The present invention is directed to a breast cancer resistance protein (BCRP/ABCG2) inhibitor. The BCRP inhibitor contains, as an active ingredient, an acrylonitrile derivative represented by formula (1): wherein one of R1 and R2 re
Efficient synthesis of N,N-disubstituted 5-aminothiophene-2-carboxaldehydes by nucleophilic aromatic substitution in water
Prim, Damien,Kirsch, Gilbert,Nicoud, Jean-Francois
, p. 383 - 384 (2007/10/03)
We have developed the first synthesis of N,N-disubstituted 5-aminothiophene-2-carboxaldehydes by Nucleophilic Aromatic Substitution of 5-bromothiophene-2-carboxaldehyde in water. This study shows selectivity between primary and secondary amines leading to