A rationally designed anticancer drug targeting a unique binding cavity of tubulin.
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.
Uckun
F M
FM
Drug Discovery Program and Parker Hughes Cancer Center, Parker Hughes Institute, St. Paul, MN 55113, USA. fatih_uckun@mercury.ih.org
Mao
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C
Vassilev
A O
AO
Navara
C S
CS
Narla
R K
RK
Jan
S T
ST
D000970:Antineoplastic Agents / Q000737:chemistry* / Q000378:metabolism / Q000494:pharmacology*; D015195:Drug Design; D004354:Drug Screening Assays, Antitumor; D005233:Fatty Alcohols / Q000737:chemistry* / Q000378:metabolism / Q000494:pharmacology*; D005663:Furans / Q000737:chemistry* / Q000378:metabolism / Q000494:pharmacology*; D006801:Humans; D008958:Models, Molecular; D011487:Protein Conformation; D014404:Tubulin / Q000737:chemistry / Q000378:metabolism*; D014407:Tumor Cells, Cultured
D000970:Antineoplastic Agents; D005233:Fatty Alcohols; D005663:Furans; D014404:Tubulin; C413724:WHI 261; C018674:tetrahydrofuran