Abstract
We report the structure-based design and synthesis of a novel series of aza-benzimidazoles as PHD2 inhibitors. These efforts resulted in compound 22, which displayed highly potent inhibition of PHD2 function in vitro.
MeSH terms
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Aza Compounds / chemical synthesis*
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Aza Compounds / chemistry
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Aza Compounds / pharmacology*
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Basic Helix-Loop-Helix Transcription Factors
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Benzimidazoles / chemical synthesis*
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Benzimidazoles / chemistry
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Benzimidazoles / pharmacology*
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Combinatorial Chemistry Techniques
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Crystallography, X-Ray
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Humans
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Hypoxia-Inducible Factor 1, alpha Subunit / antagonists & inhibitors*
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Hypoxia-Inducible Factor-Proline Dioxygenases
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Models, Molecular
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Molecular Structure
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Procollagen-Proline Dioxygenase / antagonists & inhibitors*
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Structure-Activity Relationship
Substances
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Aza Compounds
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Basic Helix-Loop-Helix Transcription Factors
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Benzimidazoles
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Hypoxia-Inducible Factor 1, alpha Subunit
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endothelial PAS domain-containing protein 1
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EGLN1 protein, human
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Procollagen-Proline Dioxygenase
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Hypoxia-Inducible Factor-Proline Dioxygenases