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Emodin (1) is the major bioactive compound of several herb species, which belongs to anthraquinone class of compound. As a part of our drug discovery program, large quantities of emodin (1) was isolated from the roots of Rheum emodi and a library of novel emodin derivatives 2–24 were prepared to evaluate their in-vitro antimalarial activity, among them, compound 17,18 and 20 showed potent antimalarial activity against chloroquine resistant strain PfK1 with the IC50 of 2.28, 2.49 and 2.48 μM respectively with a high safety index.
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