Abstract Synthesis of derivatives of diospyrin, a natural product, has led to the modification of its tumour-inhibitory effect, in vitro, towards Ehrlich ascites carcinoma and antiparasitic activity against Leishmania donovani in vitro. The present study shows that two of these novel hydroquinoid analogues derived from diospyrin also show enhanced inhibitory effects against Plasmodium falciparum, in vitro, and may be a useful model for the development of novel antimalarial drugs.