Structure-activity relationship and crystallographic studies on 4-hydroxypyrimidine HIF prolyl hydroxylase domain inhibitors
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James P Holt-Martyn Rasheduzzaman Chowdhury Anthony Tumber Tzu-Lan Yeh Martine I Abboud Kerstin Lippl Christopher T Lohans Gareth W Langley Jr Figg Michael A McDonough Christopher W Pugh Peter Ratcliffe Christopher J SchofieldAbstract
The 2-oxoglutarate-dependent hypoxia inducible factor prolyl hydroxylases (PHDs) are targets for treatment of a variety of disease states including anemia. One PHD inhibitor is approved for use in the treatment of renal anemia and others are in late stage clinical trials. However, the number of reported templates for PHD inhibition is limited. We report structure-activity relationship and crystallographic studies on a promising class of 4-hydroxypyrimidine-containing PHD inhibitors.
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Journal ChemMedChem
Volume 15
Issue number 3
Pages 270-273
Available online
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Publisher website (DOI) 10.1002/cmdc.201900557
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Europe PubMed Central 31751494
Pubmed 31751494
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