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Studies on spiro[4.5]decanone prolyl hydroxylase domain inhibitors

DOI: 10.1039/C8MD00548F DOI Help

Authors: James P. Holt-Martyn (University of Oxford) , Anthony Tumber (University of Oxford) , Mohammed Z. Rahman (University of Oxford) , Kerstin Lippl (University of Oxford) , William Figg (University of Oxford) , Michael Mcdonough (University of Oxford) , Rasheduzzaman Chowdhury (University of Oxford) , Christopher J. Schofield (University of Oxford)
Co-authored by industrial partner: No

Type: Journal Paper
Journal: Medchemcomm , VOL 10 , PAGES 500 - 504

State: Published (Approved)
Published: April 2019

Open Access Open Access

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.

Subject Areas: Chemistry, Biology and Bio-materials, Medicine

Instruments: I03-Macromolecular Crystallography

Added On: 01/03/2021 14:50


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Organic Chemistry Life Sciences & Biotech Health & Wellbeing Drug Discovery Structural biology Chemistry Biochemistry

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