Reference : Betti reaction enables efficient synthesis of 8-hydroxyquinoline inhibitors of 2-oxog...
Scientific journals : Article
Life sciences : Biochemistry, biophysics & molecular biology
Physical, chemical, mathematical & earth Sciences : Chemistry
http://hdl.handle.net/10993/26336
Betti reaction enables efficient synthesis of 8-hydroxyquinoline inhibitors of 2-oxoglutarate oxygenases.
English
Thinnes, Cyrille [University of Oxford > Department of Chemistry]
Tumber, A. [> >]
Yapp, C. [> >]
Scozzafava, G. [> >]
Yeh, T. [> >]
Chan, M. C. [> >]
Tran, T. A. [> >]
Hsu, K. [> >]
Tarhonskaya, H. [> >]
Walport, L. J. [> >]
Wilkins, S. E. [> >]
Martinez, E. D. [> >]
Muller, S. [> >]
Pugh, C. W. [> >]
Ratcliffe, P. J. [> >]
Brennan, P. E. [> >]
Kawamura, A. [> >]
Schofield, C. J. [> >]
2015
Chemical Communications
51
84
15458-61
Yes (verified by ORBilu)
International
1359-7345
1364-548X
England
[en] 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.
http://hdl.handle.net/10993/26336
10.1039/c5cc06095h

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