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Betti reaction enables efficient synthesis of 8-hydroxyquinoline inhibitors of 2-oxoglutarate oxygenases.
Thinnes, Cyrille; Tumber, A.; Yapp, C. et al.
2015In Chemical Communications, 51 (84), p. 15458-61
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Abstract :
[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.
Disciplines :
Biochemistry, biophysics & molecular biology
Chemistry
Author, co-author :
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.
More authors (8 more) Less
External co-authors :
yes
Language :
English
Title :
Betti reaction enables efficient synthesis of 8-hydroxyquinoline inhibitors of 2-oxoglutarate oxygenases.
Publication date :
2015
Journal title :
Chemical Communications
ISSN :
1364-548X
Publisher :
Royal Society of Chemistry, United Kingdom
Volume :
51
Issue :
84
Pages :
15458-61
Peer reviewed :
Peer Reviewed verified by ORBi
Available on ORBilu :
since 29 March 2016

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