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

  1. Author:
    Han, S. Q.
    Hamel, E.
    Bastow, K. F.
    McPhail, A. T.
    Brossi, A.
    Lee, K. H.

  2. Author Address

    Univ N Carolina, Sch Pharm, Nat Prod Lab, Chapel Hill, NC 27599 USA Univ N Carolina, Sch Pharm, Nat Prod Lab, Chapel Hill, NC 27599 USA NCI Frederick, Screening Technol Branch, Dev Therapeut Program, Div Canc Treatment & Diag,NIH, Frederick, MD 21702 USA Duke Univ, Dept Chem, Paul M Gross Chem Lab, Durham, NC 27708 USA Lee KH Univ N Carolina, Sch Pharm, Nat Prod Lab, Chapel Hill, NC 27599 USA
    1. Year: 2002
  2. Journal: Bioorganic & Medicinal Chemistry Letters
    1. 12
    2. 20
    3. Pages: 2851-2853
  4. Type of Article: Article
  1. 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. (C) 2002 Elsevier Science Ltd. All rights reserved.

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