Halichondrin B

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Halichondrin B Halichondrin B is the most potent member of the halichondrin family of polyether macrolides and has been isolated from several different sponge genera in extremely low yield. This high potency is exemplified by its in vivo activity against various chemoresistant human solid tumor xenografts. Binding studies showed that its mechanism of action is the inhibition of tubulin polymerization by binding near the vinca domain. Because of its potential as an effective anticancer agent, the National Cancer Institute has recommended halichondrin B for stage A clinical trials, although development has been impeded by low isolated yield from natural sources. To date several efforts has been made to address the demand for halichondrin B including aquaculture and total synthesis. Above is excerpted from Keller, Valerie; Kim, Ikyon; Burke, Steven D. Organic Letters 2005, 7, 737.