Structure-based design, synthesis, and SAR evaluation of a new series of 8-hydroxyquinolines as HIF-1α prolyl hydroxylase inhibitors
2006; Elsevier BV; Volume: 16; Issue: 21 Linguagem: Inglês
10.1016/j.bmcl.2006.08.040
ISSN1464-3405
AutoresNamal C. Warshakoon, Shengde Wu, Angelique Boyer, Richard M. Kawamoto, Justin Sheville, Sean Renock, Kevin Xu, Matthew Pokross, Songtao Zhou, Carol Winter, Richard Walter, Marlene Mekel, A.G. Evdokimov,
Tópico(s)Metal-Catalyzed Oxygenation Mechanisms
ResumoA 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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