HYDROXY-ANTHRAQUINONES AS ANTIMALARIAL AGENTS

A series of hydroxy- and polyhydroxy-anthraquinones were screened for inhibitory activity against the malarial parasite, Plasmodium falcipar um. Rufigallol demonstrated the most potent effects with a 50% inhibit ory concentration (IC50) value of similar to 10.5 ng/ml (similar to 35 nM). Deleterious effects were exerted by rufigallol toward bone marro w progenitor cells at concentrations greater than or equal to 10 mu M (3 mu g/ml) where similar to 30% suppression of colony growth was note d. Taking into consideration its potency and relative lack of toxicity , we believe that rufigallol should be advanced for in vivo studies. A t the very least, rufigallol represents a simple, inexpensive lead dru g for the development of more potent analogs.