Staff View: Evaluation of 3-carbamoylpropanoic acid analogs as inhibitors of human hypoxia-inducible factor (HIF) prolyl hydroxylase domain enzymes

Evaluation of 3-carbamoylpropanoic acid analogs as inhibitors of human hypoxia-inducible factor (HIF) prolyl hydroxylase domain enzymes

There is current interest in developing human hypoxia-inducible factor (HIF) prolyl hydroxylase domain (PHD) inhibitors for the treatment of anemia and other hypoxia-related diseases. We describe the synthesis of 3-carbamoylpropanoic acid derivatives and their evaluation as human PHD-2 inhibitors. M...

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Main Authors:	Chong, MuiPhin, Toh, LeeRoy, Tumber, Anthony, Chan, YanYing, Chan, MunChiang, Abboud, Martine I., Schofield, Christopher J., Yeoh, KarKheng
Format:	Article
Published:	Springer Verlag 2021
Subjects:	R Medicine RS Pharmacy and materia medica Pharmacopoeia
Online Access:	http://eprints.um.edu.my/33952/
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id	my.um.eprints.33952
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spelling	my.um.eprints.339522022-07-21T04:20:10Z http://eprints.um.edu.my/33952/ Evaluation of 3-carbamoylpropanoic acid analogs as inhibitors of human hypoxia-inducible factor (HIF) prolyl hydroxylase domain enzymes Chong, MuiPhin Toh, LeeRoy Tumber, Anthony Chan, YanYing Chan, MunChiang Abboud, Martine I. Schofield, Christopher J. Yeoh, KarKheng R Medicine RS Pharmacy and materia medica Pharmacopoeia There is current interest in developing human hypoxia-inducible factor (HIF) prolyl hydroxylase domain (PHD) inhibitors for the treatment of anemia and other hypoxia-related diseases. We describe the synthesis of 3-carbamoylpropanoic acid derivatives and their evaluation as human PHD-2 inhibitors. MS assays indicated that derivatives with a 3-carbamoylpropanoic acids-containing benzoxazole moiety are inhibitors of PHD-2 with IC50 values of 2.24 mu M and 1.32 mu M, respectively. However, neither the acids nor their respective ethyl esters were observed to upregulate HIF-1 alpha levels in cells. Springer Verlag 2021-04 Article PeerReviewed Chong, MuiPhin and Toh, LeeRoy and Tumber, Anthony and Chan, YanYing and Chan, MunChiang and Abboud, Martine I. and Schofield, Christopher J. and Yeoh, KarKheng (2021) Evaluation of 3-carbamoylpropanoic acid analogs as inhibitors of human hypoxia-inducible factor (HIF) prolyl hydroxylase domain enzymes. Medicinal Chemistry Research, 30 (4). pp. 977-986. ISSN 1054-2523, DOI https://doi.org/10.1007/s00044-020-02681-7 <https://doi.org/10.1007/s00044-020-02681-7>. 10.1007/s00044-020-02681-7
institution	Universiti Malaya
building	UM Library
collection	Institutional Repository
continent	Asia
country	Malaysia
content_provider	Universiti Malaya
content_source	UM Research Repository
url_provider	http://eprints.um.edu.my/
topic	R Medicine RS Pharmacy and materia medica Pharmacopoeia
spellingShingle	R Medicine RS Pharmacy and materia medica Pharmacopoeia Chong, MuiPhin Toh, LeeRoy Tumber, Anthony Chan, YanYing Chan, MunChiang Abboud, Martine I. Schofield, Christopher J. Yeoh, KarKheng Evaluation of 3-carbamoylpropanoic acid analogs as inhibitors of human hypoxia-inducible factor (HIF) prolyl hydroxylase domain enzymes
description	There is current interest in developing human hypoxia-inducible factor (HIF) prolyl hydroxylase domain (PHD) inhibitors for the treatment of anemia and other hypoxia-related diseases. We describe the synthesis of 3-carbamoylpropanoic acid derivatives and their evaluation as human PHD-2 inhibitors. MS assays indicated that derivatives with a 3-carbamoylpropanoic acids-containing benzoxazole moiety are inhibitors of PHD-2 with IC50 values of 2.24 mu M and 1.32 mu M, respectively. However, neither the acids nor their respective ethyl esters were observed to upregulate HIF-1 alpha levels in cells.
format	Article
author	Chong, MuiPhin Toh, LeeRoy Tumber, Anthony Chan, YanYing Chan, MunChiang Abboud, Martine I. Schofield, Christopher J. Yeoh, KarKheng
author_facet	Chong, MuiPhin Toh, LeeRoy Tumber, Anthony Chan, YanYing Chan, MunChiang Abboud, Martine I. Schofield, Christopher J. Yeoh, KarKheng
author_sort	Chong, MuiPhin
title	Evaluation of 3-carbamoylpropanoic acid analogs as inhibitors of human hypoxia-inducible factor (HIF) prolyl hydroxylase domain enzymes
title_short	Evaluation of 3-carbamoylpropanoic acid analogs as inhibitors of human hypoxia-inducible factor (HIF) prolyl hydroxylase domain enzymes
title_full	Evaluation of 3-carbamoylpropanoic acid analogs as inhibitors of human hypoxia-inducible factor (HIF) prolyl hydroxylase domain enzymes
title_fullStr	Evaluation of 3-carbamoylpropanoic acid analogs as inhibitors of human hypoxia-inducible factor (HIF) prolyl hydroxylase domain enzymes
title_full_unstemmed	Evaluation of 3-carbamoylpropanoic acid analogs as inhibitors of human hypoxia-inducible factor (HIF) prolyl hydroxylase domain enzymes
title_sort	evaluation of 3-carbamoylpropanoic acid analogs as inhibitors of human hypoxia-inducible factor (hif) prolyl hydroxylase domain enzymes
publisher	Springer Verlag
publishDate	2021
url	http://eprints.um.edu.my/33952/
_version_	1739828483009282048
score	13.211869

Evaluation of 3-carbamoylpropanoic acid analogs as inhibitors of human hypoxia-inducible factor (HIF) prolyl hydroxylase domain enzymes

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