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

Lookup NU author(s): Professor Akane Kawamura


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© 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.

Publication metadata

Author(s): Thinnes CC, Tumber A, Yapp C, Scozzafava G, Yeh T, Chan MC, Tran TA, Hsu K, Tarhonskaya H, Walport LJ, Wilkins SE, Martinez ED, Muller S, Pugh CW, Ratcliffe PJ, Brennan PE, Kawamura A, Schofield CJ

Publication type: Article

Publication status: Published

Journal: Chemical Communications

Year: 2015

Volume: 51

Issue: 84

Pages: 15458-15461

Print publication date: 28/10/2015

Online publication date: 28/08/2015

Acceptance date: 28/08/2015

ISSN (print): 1359-7345

ISSN (electronic): 1364-548X

Publisher: Royal Society of Chemistry


DOI: 10.1039/c5cc06095h

PubMed id: 26345662


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