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Arylthioindoles, potent inhibitors of tubulin polymerization

  1. Author:
    De Martino, G.
    La Regina, G.
    Coluccia, A.
    Edler, M. C.
    Barbera, M. C.
    Brancale, A.
    Wilcox, E.
    Hamel, E.
    Artico, M.
    Silvestri, R.

  2. Author Address

    Univ Roma La Sapienza, Dipartimento Studi Farmaceut, I-00185 Rome, Italy. Univ Wales Coll Cardiff, Welsh Sch Pharm, Cardiff CF10 3XF, S Glam, Wales. NCI, Screening Technol Branch, Dev Therapeut Program, Div Canc Treatment & Diag,NIH, Frederick, MD 21702 USA Silvestri, R, Univ Roma La Sapienza, Dipartimento Studi Farmaceut, Piazzale Aldo Moro 5, I-00185 Rome, Italy
    1. Year: 2004
    2. Date: DEC 2
  2. Journal: Journal of Medicinal Chemistry
    1. 47
    2. 25
    3. Pages: 6120-6123
  4. Type of Article: Article
  1. Abstract:

    Several arylthioindoles had excellent activity as inhibitors both of tubulin polymerization and of the growth of MCF-7 human breast carcinoma cells. Methyl 3-[(3,4,5-trimethoxyphenyl)thio]-5-methoxy-1H-indole-2-carboxylate (21), the most potent derivative, showed IC50 = 2.0 muM, 1.6 times more active than colchicine and about as active as combretastatin A-4 (CSA4). Compound 21 inhibited the growth of the MCF-7 cells at IC50 = 13 nM. Colchicine and CSA4 had 13 nM and 17 nM IC50 values, respectively, with these cells

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External Sources

  1. View record in Web of Science®
  2. WOS: 000225409400003

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