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Issue 4, 2019
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Studies on spiro[4.5]decanone prolyl hydroxylase domain inhibitors

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Abstract

The 2-oxoglutarate (2OG) dependent hypoxia inducible factor (HIF) prolyl hydroxylases (PHDs) are targets for treatment of anaemia and other ischaemia related diseases. PHD inhibitors are in clinical trials; however, the number of reported templates for PHD inhibition is limited. We report structure–activity relationship and crystallographic studies on spiro[4.5]decanone containing PHD inhibitors. Together with other studies, our results reveal spiro[4.5]decanones as useful templates for generation of potent and selective 2OG oxygenase inhibitors.

Graphical abstract: Studies on spiro[4.5]decanone prolyl hydroxylase domain inhibitors

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Publication details

The article was received on 05 Nov 2018, accepted on 09 Feb 2019 and first published on 01 Mar 2019


Article type: Review Article
DOI: 10.1039/C8MD00548F
Citation: Med. Chem. Commun., 2019,10, 500-504
  • Open access: Creative Commons BY license
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    Studies on spiro[4.5]decanone prolyl hydroxylase domain inhibitors

    J. P. Holt-Martyn, A. Tumber, M. Z. Rahman, K. Lippl, W. Figg, M. A. McDonough, R. Chowdhury and C. J. Schofield, Med. Chem. Commun., 2019, 10, 500
    DOI: 10.1039/C8MD00548F

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