The synthesis of morusin as a potent antitumor agent

Morusin, which can be isolated from Chinese herbal medicine, is achieved in which the longest linear sequence is only 13 steps in 12% overall yield from commercially available phloroglucinol. In addition, the metal/EtSH reagents for regioselective demethylation of polymethylated morusin were described. Consequently, this strategy provided a concise route to synthesize the morusin analogues as well. Further biological studies of morusin, it exhibited strong antitumor effects with IC50 ∼3.0 μM on three cancer cells.

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