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.

Original publication

DOI

10.1039/c5cc06095h

Type

Journal article

Journal

Chem Commun (Camb)

Publication Date

28/10/2015

Volume

51

Pages

15458 - 15461

Keywords

Dose-Response Relationship, Drug, Enzyme Inhibitors, Humans, Models, Molecular, Molecular Structure, Oxygenases, Oxyquinoline, Structure-Activity Relationship