A rationally designed anticancer drug targeting a unique binding cavity of tubulin.

F M Uckun, C Mao, A O Vassilev, C S Navara, R K Narla, S T Jan

Drug Discovery Program and Parker Hughes Cancer Center, Parker Hughes Institute, St. Paul, MN 55113, USA. fatih_uckun@mercury.ih.org

Bioorganic & medicinal chemistry letters 2000 May 15

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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.

Citation

F M Uckun, C Mao, A O Vassilev, C S Navara, R K Narla, S T Jan. A rationally designed anticancer drug targeting a unique binding cavity of tubulin. Bioorganic & medicinal chemistry letters. 2000 May 15;10(10):1015-8