2. Academic Validation
  3. Antitumor agents. Part 215: antitubulin effects of cytotoxic B-ring modified allocolchicinoids

Antitumor agents. Part 215: antitubulin effects of cytotoxic B-ring modified allocolchicinoids

  • Bioorg Med Chem Lett. 2002 Oct 21;12(20):2851-3. doi: 10.1016/s0960-894x(02)00635-2.
Shiqing Han 1,  Ernest Hamel,  Kenneth F Bastow,  Andrew T McPhail,  Arnold Brossi,  Kuo-Hsiung Lee
Affiliations

Affiliation

  • 1 Natural Products Laboratory, School of Pharmacy, University of North Carolina at Chapel Hill, NC 27599, USA.
PMID: 12270161 DOI: 10.1016/s0960-894x(02)00635-2
Abstract

N-Acetylcolchinol methyl ether 1 served as the starting material to prepare the chloroacetamide (3) and epoxide (5) analogues. Both 3 and 5 were potent inhibitors of tubulin polymerization in vitro. Compound 3 was also 4-fold more cytotoxic than colchicine against the 1A9 tumor cell line and showed a unique cross-resistance profile.

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