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

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.

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