Structure-activity relationship for branched oxyquinoline HIF activators: Effect of modifications to phenylacetamide “tail”

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• 作者：A.A. Poloznikov^a ; ^{andrey.poloznikov@gmail.com} ; A.A. Zakhariants^b ; S.V. Nikulin^a ; ^c ; N.A. Smirnova^a ; D.M. Hushpulian^a ; I.N. Gaisina^d ; A.G. Tonevitsky^b ; V.I. Tishkov^e ; ^f ; ^g ; I.G. Gazaryan^a ; ^f
• 关键词：7-Substituted 8-hydroxyquinoline ; HIF prolyl hydroxylase ; HIF1 ODD-luc reporter ; Luciferase assay ; Liver-on-a-chip ; Hepatotoxicity
• 刊名：Biochimie
• 出版年：2017
• 出版时间：February 2017
• 年：2017
• 卷：133
• 期：Complete
• 页码：74-79
• 全文大小：705 K
• 卷排序：133

文摘

25 “branched tail” oxyquinoline HIF activators were tested in ODD-luc reporter assay. The activation effect is sensitive to 5-Cl-substitution in the oxyquinoline ring. A 3-fold more potent HIF activator than the original compound has been identified. The oxyquinolines show no toxicity in “liver-on-a-chip” up to 200 μM concentration.