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.
Full text not available from this repository.Abstract
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.
| Item Type: | Article |
|---|---|
| Funders: | Universiti Sains Malaysia[1001.PKIMIA.811250], Bantuan Kecil Penyelidikan, University of Malaya[BKP004-2018], Wellcome Trust, Cancer Research UK |
| Uncontrolled Keywords: | Hypoxia-inducible factor;HIF;Prolyl hydroxylase domain;PHD inhibitors;2-oxoglutarate;Alpha-ketoglutarate dependent oxygenase;3-carbamoylpropanoic acid derivatives |
| Subjects: | R Medicine R Medicine > RS Pharmacy and materia medica R Medicine > RS Pharmacy and materia medica > Pharmacopoeia |
| Divisions: | Faculty of Medicine |
| Depositing User: | Ms Zaharah Ramly |
| Date Deposited: | 21 Jul 2022 04:20 |
| Last Modified: | 21 Jul 2022 04:20 |
| URI: | http://eprints.um.edu.my/id/eprint/33952 |
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