Bioorganic and Medicinal Chemistry Letters 2000-May
A rationally designed anticancer drug targeting a unique binding cavity of tubulin.
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A novel mono-THF containing synthetic anticancer drug (WHI-261) was designed for targeting a previously unrecognized unique narrow binding cavity on the surface of tubulin. The anti-cancer activity of WHI-261 was confirmed using MTT assays. The structure-based design, synthesis, and biological activity of WHI-261 are reported.