Studies on spiro[4.5]decanone prolyl hydroxylase domain inhibitors.
Journal
MedChemComm
ISSN: 2040-2511
Titre abrégé: Medchemcomm
Pays: England
ID NLM: 101531525
Informations de publication
Date de publication:
01 Apr 2019
01 Apr 2019
Historique:
received:
05
11
2018
accepted:
09
02
2019
entrez:
7
5
2019
pubmed:
7
5
2019
medline:
7
5
2019
Statut:
epublish
Résumé
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.
Identifiants
pubmed: 31057728
doi: 10.1039/c8md00548f
pii: c8md00548f
pmc: PMC6482412
doi:
Types de publication
Journal Article
Review
Langues
eng
Pagination
500-504Subventions
Organisme : Wellcome Trust
Pays : United Kingdom
Organisme : British Heart Foundation
ID : PG/12/33/29546
Pays : United Kingdom
Organisme : British Heart Foundation
ID : RE/13/1/30181
Pays : United Kingdom
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