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

[ Vol. 12 , Issue. 4 ]

Author(s):

Yan Xia, Qiong Duan, Bao-Hua Zhao, Dong-Feng Li and Rui-Bin Hou   Pages 338 - 346 ( 9 )

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.

Affiliation:

Laboratory of Photoelectric Material, Advanced Institute of Materials Science, Changchun University of Technology, 130012, Changchun, P. R. China., Department of Chemistry, College of Chemistry and Life Science, Changchun University of Technology, 130012, Changchun, P. R. China.



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