Jump to main content
Jump to site search

Issue 84, 2015
Previous Article Next Article

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

Author affiliations

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

Back to tab navigation

Supplementary files

Article information


Submitted
21 Jul 2015
Accepted
28 Aug 2015
First published
28 Aug 2015

Chem. Commun., 2015,51, 15458-15461
Article type
Communication
Author version available

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

Social activity

Search articles by author

Spotlight

Advertisements