Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 16, Issue 21, Pages 5517-5522Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2006.08.040
Keywords
prolyl hydroxylase inhibitors; HIF-1 alpha; hypoxia; ischemia; peripheral arterial disease (PAD); anemia; 8-hydroxyquinolinecarboxyamides
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A new series of potent 8-hydroxyquinolines was designed based on the newly resolved X-ray crystal structure of EGLN-1. Both alkyl and aryl 8-hydroxyquinoline-7-carboxyamides were good HIF-1 alpha prolyl hydroxylase (EGLN) inhibitors. In subsequent VEGF induction assays, these exhibited potent VEGF activity. In addition, this class of compounds did show the ability to stabilize HIF-1 alpha. (c) 2006 Elsevier Ltd. All rights reserved.
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