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.
Rights & PermissionsPrintExport