Betti reaction enables efficient synthesis of 8-hydroxyquinoline inhibitors of 2-oxoglutarate oxygenases
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CC Thinnes A Tumber C Yapp G Scozzafava T Yeh MC Chan TA Tran K Hsu H Tarhonskaya Louise Walport SE Wilkins ED Martinez S Müller CW Pugh Peter Ratcliffe PE Brennan A Kawamura CJ SchofieldAbstract
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.
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Journal Chemical Communications
Volume 51
Issue number 84
Pages 15458-15461
Available online
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Publisher website (DOI) 10.1039/c5cc06095h
Europe PubMed Central 26345662
Pubmed 26345662
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