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Studies on spiro[4.5]decanone prolyl hydroxylase domain inhibitors

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 gener...

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Publication status:
Published
Peer review status:
Peer reviewed

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Files:
Publisher copy:
10.1039/c8md00548f

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More by this author
Institution:
University of Oxford
Division:
MPLS Division
Department:
Chemistry
Sub department:
Organic Chemistry
Role:
Author
More by this author
Institution:
University of Oxford
Division:
MPLS Division
Department:
Chemistry
Sub department:
Organic Chemistry
Role:
Author
More by this author
Institution:
University of Oxford
Division:
MPLS Division
Department:
Chemistry
Sub department:
Organic Chemistry
Role:
Author
More by this author
Institution:
University of Oxford
Division:
MPLS Division
Department:
Chemistry
Sub department:
Organic Chemistry
Role:
Author
More by this author
Institution:
University of Oxford
Division:
MPLS Division
Department:
Chemistry
Sub department:
Organic Chemistry
Role:
Author
More from this funder
Name:
Cancer Research UK
Grant:
18245
More from this funder
Name:
British Heart Foundation
Grant:
PG/12/33/29546
More from this funder
Name:
Wellcome Trust
Grant:
106244/Z/14/Z
Publisher:
Royal Society of Chemistry
Journal:
MedChemComm More from this journal
Volume:
2019
Issue:
4
Article number:
500
Publication date:
2019-03-01
Acceptance date:
2019-02-09
DOI:
EISSN:
2040-2511
ISSN:
2040-2503
Pubs id:
pubs:975034
UUID:
uuid:063de5c2-f147-41cd-babe-e20d8673d91e
Local pid:
pubs:975034
Deposit date:
2019-02-21

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