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Studies on spiro[4.5]decanone prolyl hydroxylase domain inhibitors
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–...
| Autores principales: | , , , , , , , |
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| Formato: | Online Artículo Texto |
| Lenguaje: | English |
| Publicado: |
Royal Society of Chemistry
2019
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| Materias: | |
| Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6482412/ https://www.ncbi.nlm.nih.gov/pubmed/31057728 http://dx.doi.org/10.1039/c8md00548f |
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| author | Holt-Martyn, James P. Tumber, Anthony Rahman, Mohammed Z. Lippl, Kerstin Figg, William McDonough, Michael A. Chowdhury, Rasheduzzaman Schofield, Christopher J. |
| author_facet | Holt-Martyn, James P. Tumber, Anthony Rahman, Mohammed Z. Lippl, Kerstin Figg, William McDonough, Michael A. Chowdhury, Rasheduzzaman Schofield, Christopher J. |
| author_sort | Holt-Martyn, James P. |
| collection | PubMed |
| description | 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. |
| format | Online Article Text |
| id | pubmed-6482412 |
| institution | National Center for Biotechnology Information |
| language | English |
| publishDate | 2019 |
| publisher | Royal Society of Chemistry |
| record_format | MEDLINE/PubMed |
| spelling | pubmed-64824122019-06-28 Studies on spiro[4.5]decanone prolyl hydroxylase domain inhibitors Holt-Martyn, James P. Tumber, Anthony Rahman, Mohammed Z. Lippl, Kerstin Figg, William McDonough, Michael A. Chowdhury, Rasheduzzaman Schofield, Christopher J. Medchemcomm Chemistry 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. Royal Society of Chemistry 2019-03-01 /pmc/articles/PMC6482412/ /pubmed/31057728 http://dx.doi.org/10.1039/c8md00548f Text en This journal is © The Royal Society of Chemistry 2019 http://creativecommons.org/licenses/by/3.0/ This article is freely available. This article is licensed under a Creative Commons Attribution 3.0 Unported Licence (CC BY 3.0) |
| spellingShingle | Chemistry Holt-Martyn, James P. Tumber, Anthony Rahman, Mohammed Z. Lippl, Kerstin Figg, William McDonough, Michael A. Chowdhury, Rasheduzzaman Schofield, Christopher J. Studies on spiro[4.5]decanone prolyl hydroxylase domain inhibitors |
| title | Studies on spiro[4.5]decanone prolyl hydroxylase domain inhibitors
|
| title_full | Studies on spiro[4.5]decanone prolyl hydroxylase domain inhibitors
|
| title_fullStr | Studies on spiro[4.5]decanone prolyl hydroxylase domain inhibitors
|
| title_full_unstemmed | Studies on spiro[4.5]decanone prolyl hydroxylase domain inhibitors
|
| title_short | Studies on spiro[4.5]decanone prolyl hydroxylase domain inhibitors
|
| title_sort | studies on spiro[4.5]decanone prolyl hydroxylase domain inhibitors |
| topic | Chemistry |
| url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6482412/ https://www.ncbi.nlm.nih.gov/pubmed/31057728 http://dx.doi.org/10.1039/c8md00548f |
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