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Synthesis and biological evaluation of 2-and 3-aminobenzo b thiophene derivatives as antimitotic agents and inhibitors of tubulin polymerization

  1. Author:
    Romagnoli, R.
    Baraldi, P. G.
    Carrion, M. D.
    Cara, C. L.
    Preti, D.
    Fruttarolo, F.
    Pavani, M. G.
    Tabrizi, M. A.
    Tolomeo, M.
    Grimaudo, S.
    Di Cristina, A.
    Balzarini, J.
    Hadfield, J. A.
    Brancale, A.
    Hamel, E.

  2. Author Address

    Univ Ferrara, Dipartimento Sci Farmaceut, I-44100 Ferrara, Italy. Univ Palermo, Policlin P Giaccone, Div Ematol, Palermo, Italy. Univ Palermo, Policlin P Giaccone, Serv AIDS, Palermo, Italy. Catholic Univ Louvain, Rega Inst Med Res, Lab Virol & Chemotherapy, B-3000 Louvain, Belgium. Univ Salford, Ctr Mol Drug Design, Salford M5 4W5, Lancs, England. Univ Cardiff Wales, Welsh Sch Pharm, Cardiff CF10 3XF, Wales. NCI, Frederick Canc Res & Dev Ctr, Div Canc Treatment & Diag,Dev Therapeut Program, Toxicol & Pharmacol Branch,NIH, Frederick, MD 21702 USA.;Romagnoli, R, Univ Ferrara, Dipartimento Sci Farmaceut, I-44100 Ferrara, Italy.;rmr@unife.it baraldi@unife.it
    1. Year: 2007
    2. Date: May
  2. Journal: Journal of Medicinal Chemistry
    1. 50
    2. 9
    3. Pages: 2273-2277
  4. Type of Article: Article
  5. ISSN: 0022-2623
  1. Abstract:

    Two new series of inhibitors of tubulin polymerization based on the 2-amino-3-(3,4,5-trimethoxybenzoyl)benzo[b]thiophene molecular skeleton and its 3-amino positional isomer were synthesized and evaluated for antiproliferative activity, inhibition of tubulin polymerization, and cell cycle effects. Although many more 3-amino derivatives have been synthesized so far, the most promising compound in this series was 2-amino-6-methyl-3-(3,4,5-trimethoxybenzoyl)benzo[b]thiophene, which inhibits cancer cell growth at subnanomolar concentrations and interacts strongly with tubulin by binding to the colchicine site.

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External Sources

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  2. DOI: 10.1021/jm070050f
  3. View record in Web of Science®
  4. WOS: 000245954600033

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