Synthesis of dihydrolucilactaene: a newly discoveredantimalarial compound

Abstract

The discovery of dihydrolucilactaene as a secondary metabolite in fungus Fusarium sp. RK97-94 showed a 100-fold increase in potency in antimalarial activity compared with its analoguelucilactaene. Although dihydrolucilactaene shows a high level of antimalarial activity and had been shown to be a promising drug lead candidate for malaria treatment due to its highly selective cytotoxicity towards malaria-causing pathogens and negligible cytotoxicity towards other cells at lower concentrations, its complete biosynthesis pathway in Fusarium sp. RK97-94 is still to be determined, making mass production of the molecule via biological means less than desirable. In this work, we propose a complete chemical synthesis route for dihydrolucilactaene via a series of reactions involving commercially available reagents for the potential industrial application and mass production of dihydrolucilactaene.