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Antitumor agents. 192. Antitubulin effect and cytotoxicity of C(7)-oxygenated allocolchicinoids

  1. Author:
    Guan, J.
    Zhu, X. K.
    Brossi, A.
    Tachibana, Y.
    Bastow, K. F.
    Verdier-Pinard, P.
    Hamel, E.
    McPhail, A. T.
    Lee, K. H.
  2. Author Address

    Lee KH Univ N Carolina, Sch Pharm, Div Med Chem & Nat Prod, Nat Prod Lab Chapel Hill, NC 27599 USA Univ N Carolina, Sch Pharm, Div Med Chem & Nat Prod, Nat Prod Lab Chapel Hill, NC 27599 USA NCI, Lab Drug Discovery Res & Dev, Dev Therapeut Program, Frederick Canc Res & Dev Ctr Frederick, MD 21702 USA Duke Univ, Paul M Gross Chem Lab Durham, NC 27708 USA
    1. Year: 1999
  1. Journal: Collection of Czechoslovak Chemical Communications
    1. 64
    2. 2
    3. Pages: 217-228
  2. Type of Article: Article
  1. Abstract:

    Two allocolchicinoids 6 and 8, prepared from colchicine, together with allo compounds 9-11, made from 6 by reduction and regiodemethylation, were evaluated for antitubulin and antitumor activities. Structures of 6, 8, and 10 were confirmed by X-ray crystallographic analysis. Compounds 6, 8, and 9 have high tubulin binding affinity and display potent inhibitory activities against tubulin polymerization and solid human tumor cell lines. Particularly, drug-resistant KB cell lines, including KB-7d, KB-VCR, and KB-CPT, do not show marked resistance to these compounds. [References: 23]

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