Abstract
Hypoxia inducible factor-1 (HIF-1) is a key mediator during cancer cells to adapt tumor hypoxic condition. In this study, a series of adamantane-based compounds were synthesized and evaluated as potential inhibitors of HIF-1α. Examination of their structure-activity relationship (SAR) identified the adamantane-containing indole derivative 20a as a potent inhibitor of HIF-1α in Hep3B cell lines under tumor hypoxia (IC50 = 0.02 µM). The study herein may provide valuable information for the development of novel therapeutics against cancer and tumor angiogenesis.
Keywords: Adamantane, hypoxia inducible factor-1, structure-activity relationship, tumor angiogenesis.
Medicinal Chemistry
Title:Design, Synthesis and Structure-Activity Relationship Studies of Novel 4 (1-adamantyl) Phenyl Analogues as HIF-1α Inhibitors
Volume: 12 Issue: 4
Author(s): Yan Xia, Qiong Duan, Bao-Hua Zhao, Dong-Feng Li and Rui-Bin Hou
Affiliation:
Keywords: Adamantane, hypoxia inducible factor-1, structure-activity relationship, tumor angiogenesis.
Abstract: Hypoxia inducible factor-1 (HIF-1) is a key mediator during cancer cells to adapt tumor hypoxic condition. In this study, a series of adamantane-based compounds were synthesized and evaluated as potential inhibitors of HIF-1α. Examination of their structure-activity relationship (SAR) identified the adamantane-containing indole derivative 20a as a potent inhibitor of HIF-1α in Hep3B cell lines under tumor hypoxia (IC50 = 0.02 µM). The study herein may provide valuable information for the development of novel therapeutics against cancer and tumor angiogenesis.
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Cite this article as:
Xia Yan, Duan Qiong, Zhao Bao-Hua, Li Dong-Feng and Hou Rui-Bin, Design, Synthesis and Structure-Activity Relationship Studies of Novel 4 (1-adamantyl) Phenyl Analogues as HIF-1α Inhibitors, Medicinal Chemistry 2016; 12 (4) . https://dx.doi.org/10.2174/1573406412666151109113007
DOI https://dx.doi.org/10.2174/1573406412666151109113007 |
Print ISSN 1573-4064 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-6638 |
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