Zerumbone, a sesquiterpene isolated from the rhizome of Zingiber zerumbet, shows strong antimalarial and cytotoxic activities. A series of zerumbone derivatives were synthesized and evaluated for in vitro antimalarial activity against Plasmodium falciparum and cytotoxicity against human cancer cell lines (NCI-H187, KB and BC) as well as normal cells (Vero cells). Three of the compounds showed potent antimalarial activity with IC50 values of 32.8, 13.7, and 9.8 μM. They were less toxic against Vero cells.
