This review involves the chemistry and biochemistry of lapachol, β-lapachone and
lawsone, examples of bioactive natural products that still being under biological evaluation and
stimulated several research groups to prepare derivatives and analogues and test them against
several anticancer, trypanocidal, antinflammatory, tuberculostatic, and antimalarial targets, as
well as other parasitology targets related to important infectious diseases.
Keywords: β-lapachone, lapachol, lawsone, derivatives, biological activities,
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