Abstract
Utilizing modeling information from a recently resolved structure of human HIF-1alpha prolyl hydroxylase (EGLN1) and structure-based design, a novel series of imidazo[1,2-a]pyridine derivatives was prepared. The activity of these compounds was determined in a human EGLN1 assay and a limited SAR was developed.
MeSH terms
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Humans
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Hypoxia-Inducible Factor-Proline Dioxygenases
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Procollagen-Proline Dioxygenase / antagonists & inhibitors*
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Pyridines / pharmacology*
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Structure-Activity Relationship
Substances
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Pyridines
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EGLN1 protein, human
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Procollagen-Proline Dioxygenase
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Hypoxia-Inducible Factor-Proline Dioxygenases
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imidazo(1,2-a)pyridine