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Antitumo agents 238. Anti-tubulin and in vitro cytotoxic effects of N-substituted allocolchicinoids

  1. Author:
    Nakagawa-Goto, K.
    Jung, M. K.
    Hamel, E.
    Wu, C. C.
    Bastow, K. F.
    Brossi, A.
    Ohta, S.
    Lee, K. H.

  2. Author Address

    Univ N Carolina, Sch Pharm, Nat Prod Lab, Chapel Hill, NC 27599 USA. SAIC Frederick Inc, Ft Detrick, MD 21702 USA. Natl Canc Inst, Screening Technol Branch, Dev Therapeut Program, Div Canc Treatment & Diag,NIH, Ft Detrick, MD 21702 USA. Kyoto Pharmaceut Univ, Kyoto 6078414, Japan Nakagawa-Goto, K, Univ N Carolina, Sch Pharm, Nat Prod Lab, Chapel Hill, NC 27599 USA
    1. Year: 2005
  2. Journal: Heterocycles
    1. 65
    2. 3
    3. Pages: 541-550
  4. Type of Article: Article
  1. Abstract:

    (-)-N-Substituted colchinol methyl ethers (6-10) and N-alkyl HCl salts (8a-10a) were synthesized from (-)-colchicine (1). The new compounds were evaluated for in vitro cytotoxic activity against five human tumor cell lines and for inhibition of tubulin polymerization. The new carbamate (6) and amide (7) showed 10-fold stronger activity against human tumor cell line replication than the amines (8-10). The corresponding HCl salts (8a-10a) generally showed decreased activity. Compounds (6) and (7) also exerted strong inhibitory effects on tubulin polymerization. All of the colchinol methyl ethers showed essentially equal cytotoxic effects against MDR-resistant (KB-V) and non-resistant (KB) cells, while the potency of colchicine was decreased 100-fold against KB-V cells

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External Sources

  1. View record in Web of Science®
  2. WOS: 000228034700004

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