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

Abstract

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.

• Authors: F M Uckun, C Mao, A O Vassilev, C S Navara, R K Narla, S T Jan
• Journal: Bioorganic & medicinal chemistry letters (Bioorg Med Chem Lett) Vol. 10 Issue 10 Pg. 1015-8 (May 15 2000) ISSN: 0960-894X [Print] England
• PMID: 10843205 (Publication Type: Journal Article)

Chemical References

• Antineoplastic Agents
• Fatty Alcohols
• Furans
• Tubulin
• WHI 261
• tetrahydrofuran

Topics

• Antineoplastic Agents (chemistry, metabolism, pharmacology)
• Drug Design
• Drug Screening Assays, Antitumor
• Fatty Alcohols (chemistry, metabolism, pharmacology)
• Furans (chemistry, metabolism, pharmacology)
• Humans
• Models, Molecular
• Protein Conformation
• Tubulin (chemistry, metabolism)
• Tumor Cells, Cultured