Structure-based design, synthesis, and SAR evaluation of a new series of 8-hydroxyquinolines as HIF-1α prolyl hydroxylase inhibitors

Article ID	Journal	Published Year	Pages	File Type
1376487	Bioorganic & Medicinal Chemistry Letters	2006	6 Pages	PDF

Abstract

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-1α 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-1α.

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Keywords

HIF-1?Ischemia Peripheral arterial disease (PAD)Prolyl hydroxylase inhibitors Hypoxia Anemia

Related Topics

Physical Sciences and Engineering Chemistry Organic Chemistry

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Structure-based design, synthesis, and SAR evaluation of a new series of 8-hydroxyquinolines as HIF-1α prolyl hydroxylase inhibitors

Authors

Namal C. Warshakoon, Shengde Wu, Angelique Boyer, Richard Kawamoto, Justin Sheville, Sean Renock, Kevin Xu, Matthew Pokross, Songtao Zhou, Carol Winter, Richard Walter, Marlene Mekel, Artem G. Evdokimov,