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Synthesis of novel pyridine-carboxylates as small-molecule inhibitors of human aspartate/asparagine-β-hydroxylase

Abstract:

The human 2-oxoglutarate (2OG)-dependent oxygenase aspartate/asparagine-β-hydroxylase (AspH) is a potential medicinal chemistry target for anti-cancer therapy. AspH is overexpressed on the cell surface of invasive cancer cells and accepts epidermal growth factor-like domain (EGFDs) substrates with a non-canonical ( i.e. Cys 1-2, 3-4, 5-6) disulfide pattern. We report a concise synthesis of C-3 substituted derivatives of pyridine-2,4-dicarboxylic acid (2,4-PDCA) as 2OG competitors for us...

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Publication status:
Published
Peer review status:
Peer reviewed

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Publisher copy:
10.1002/cmdc.202000147

Authors


More by this author
Institution:
University of Oxford
Division:
MPLS
Department:
Chemistry
Role:
Author
More by this author
Institution:
University of Oxford
Division:
MPLS
Department:
Chemistry
Role:
Author
More by this author
Institution:
University of Oxford
Division:
MPLS
Department:
Chemistry
Role:
Author
More by this author
Institution:
University of Oxford
Division:
MPLS
Department:
Chemistry
Role:
Author
ORCID:
0000-0001-7552-4966
More by this author
Institution:
University of Oxford
Division:
MPLS
Department:
Chemistry
Role:
Author
Publisher:
Wiley Publisher's website
Journal:
ChemMedChem Journal website
Volume:
15
Issue:
2020
Pages:
1139 –1149
Publication date:
2020-04-24
Acceptance date:
2020-04-21
DOI:
EISSN:
1860-7187
ISSN:
1860-7179
Pmid:
32330361

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