Brennan PE

Chan MC

Hsu K

Kawamura A

Martinez ED

Muller S

Pugh CW

Ratcliffe PJ

Schofield CJ

Scozzafava G

Tarhonskaya H

Thinnes CC

Tran TA

Tumber A

Walport LJ

Wilkins SE

Yapp C

Yeh T

\ua9 The Royal Society of Chemistry 2015. 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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Betti reaction enables efficient synthesis of 8-hydroxyquinoline inhibitors of 2-oxoglutarate oxygenases

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

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