Design, Synthesis and Structure-Activity Relationship Studies of Novel 4 (1-adamantyl) Phenyl Analogues as HIF-1α Inhibitors

Author(s): Yan Xia, Qiong Duan, Bao-Hua Zhao, Dong-Feng Li, Rui-Bin Hou.

Journal Name: Medicinal Chemistry

Volume 12 , Issue 4 , 2016

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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.

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Article Details

VOLUME: 12
ISSUE: 4
Year: 2016
Page: [338 - 346]
Pages: 9
DOI: 10.2174/1573406412666151109113007
Price: $65

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