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Symmetrical alpha-bromoacryloylamido diaryldienone derivatives as a novel series of antiproliferative agents. Design, synthesis and biological evaluation

  1. Author:
    Romagnoli, R.
    Baraldi, P. G.
    Cruz-Lopez, O.
    Cara, C. L.
    Carrion, M. D.
    Balzarini, J.
    Hamel, E.
    Basso, G.
    Bortolozzi, R.
    Viola, G.

  2. Author Address

    [Romagnoli, Romeo; Baraldi, Pier Giovanni; Cruz-Lopez, Olga; Cara, Carlota Lopez; Carrion, Maria Dora] Univ Ferrara, Dipartimento Sci Farmaceut, I-44100 Ferrara, Italy. [Balzarini, Jan] Catholic Univ Louvain, Rega Inst Med Res, Lab Virol & Chemotherapy, B-3000 Louvain, Belgium. [Hamel, Ernest] NCI, Screening Technol Branch, Dev Therapeut Program, Div Canc Treatment & Diag,NIH, Frederick, MD 21702 USA. [Basso, Giuseppe; Bortolozzi, Roberta; Viola, Giampietro] Univ Padua, Dipartimento Pediat, Lab Oncoematol, I-35131 Padua, Italy.;Romagnoli, R, Univ Ferrara, Dipartimento Sci Farmaceut, I-44100 Ferrara, Italy.;rmr@unife.it baraldi@unife.it
    1. Year: 2010
    2. Date: May
  2. Journal: Bioorganic & Medicinal Chemistry Letters
    1. 20
    2. 9
    3. Pages: 2733-2739
  4. Type of Article: Article
  5. ISSN: 0960-894X
  1. Abstract:

    In a continuing study of hybrid compounds containing the alpha-bromoacryloyl moiety as potential anticancer drugs, we synthesized a novel series of hybrids 4a-h, in which this moiety was linked to a 1,5-diaryl-1,4-pentadien-3-one system. Many of the conjugates prepared (4b, 4c, 4e and 4g) demonstrated pronounced, submicromolar antiproliferative activity against four cancer cell lines. Moreover, compound 4b induced apoptosis through the mitochondrial pathway and activated caspase-3 in a concentration-dependent manner. (C) 2010 Elsevier Ltd. All rights reserved.

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External Sources

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  2. DOI: 10.1016/j.bmcl.2010.03.075
  3. View record in Web of Science®
  4. WOS: 000276816600008

Library Notes

  1. Fiscal Year: FY2009-2010
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