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Issue 84, 2015
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Betti reaction enables efficient synthesis of 8-hydroxyquinoline inhibitors of 2-oxoglutarate oxygenases

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Abstract

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.

Graphical abstract: Betti reaction enables efficient synthesis of 8-hydroxyquinoline inhibitors of 2-oxoglutarate oxygenases

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Publication details

The article was received on 21 Jul 2015, accepted on 28 Aug 2015 and first published on 28 Aug 2015


Article type: Communication
DOI: 10.1039/C5CC06095H
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Citation: Chem. Commun., 2015,51, 15458-15461
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    Betti reaction enables efficient synthesis of 8-hydroxyquinoline inhibitors of 2-oxoglutarate oxygenases

    C. C. Thinnes, A. Tumber, C. Yapp, G. Scozzafava, T. Yeh, M. C. Chan, T. A. Tran, K. Hsu, H. Tarhonskaya, L. J. Walport, S. E. Wilkins, E. D. Martinez, S. Müller, C. W. Pugh, P. J. Ratcliffe, P. E. Brennan, A. Kawamura and C. J. Schofield, Chem. Commun., 2015, 51, 15458
    DOI: 10.1039/C5CC06095H

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