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New arylthioindoles: Potent inhibitors of tubulin polymerization. 2. Structure-activity relationships and molecular modeling studies

  1. Author:
    De Martino, G.
    Edler, M. C.
    La Regina, G.
    Coluccia, A.
    Barbera, M. C.
    Barrow, D.
    Nicholson, R. I.
    Chiosis, G.
    Brancale, A.
    Hamel, E.
    Artico, M.
    Silvestri, R.

  2. Author Address

    Univ Roma La Sapienza, Dipartimento Studi Farmaceut, Fdn Cenci Bolognetti, Ist Pasteur, I-00185 Rome, Italy. Univ Cardiff Wales, Welsh Sch Pharm, Cardiff CF10 3XF, Wales. Mem Sloan Kettering Canc Ctr, Cell Biol Program, New York, NY 10021 USA. NCI, Toxicol & Pharmacol Branch, Dev Therapeut Program, Div Canc Treatment & Diag,NIH, Frederick, MD 21702 USA. Univ Cardiff Wales, Welsh Sch Pharm, Tenovus Ctr Canc Res, Cardiff CF10 3XF, Wales Silvestri, R, Univ Roma La Sapienza, Dipartimento Studi Farmaceut, Fdn Cenci Bolognetti, Ist Pasteur, Piazzale Aldo Moro 5, I-00185 Rome, Italy
    1. Year: 2006
    2. Date: FEB 9
  2. Journal: Journal of Medicinal Chemistry
    1. 49
    2. 3
    3. Pages: 947-954
  4. Type of Article: Article
  1. Abstract:

    Arylthioindoles (ATIs) that possess a 3-methoxyphenylthio or a 3,5-dimethoxyphenylthio moiety at position 2 of the indole ring were effective tubulin assembly inhibitors, but weak inhibitors of MCF-7 cell growth. ATIs bearing a 3-(3,4,5-trimethoxyphenyl)thio moiety were potent tubulin polymerization inhibitors, with IC(50)s in the 2.0 (35) to 4.5 (37) mu M range. They also inhibited MCF-7 cell growth at nanomolar concentrations. The 3,4,5-trimethoxy substituted ATIs showed potencies comparable to those of the reference compounds colchicine and combretastatin A-4 in both tubulin assembly and cell growth inhibition assays. Dynamics simulation studies correlate well with the observed experimental data. Furthermore, from careful analysis of the biological and in silico data, we can now hypothesize a basic pharmacophore for this class of compounds

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  2. WOS: 000235826300014

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