HIF-1α inhibitors: Synthesis and biological evaluation of novel moracin O and P analogues

► Natural products, moracins O and P, as leads for development of HIF-1α inhibitor. ► We examined structure-activity relationship study of benzofuran based moracin derivatives using cell-based HRE assay. ► The primary activity of the represented compound was confirmed by biochemical methods. ► In this study we conclude that 2-arylbenzofuran ring and the (R)-configuration of the core scaffold is important for activity.