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Substituted E-3-(3-Indolylmethylene)-1,3-dihydroindo1-2-ones with Antitumor Activity. In Depth Study of the Effect on Growth of Breast Cancer Cells

  1. Author:
    Andreani, A.
    Bellini, S.
    Burnelli, S.
    Granaiola, M.
    Leoni, A.
    Locatelli, A.
    Morigi, R.
    Rambaldi, M.
    Varoli, L.
    Calonghi, N.
    Cappadone, C.
    Zini, M.
    Stefanelli, C.
    Masotti, L.
    Shoemaker, R. H.

  2. Author Address

    [Andreani, Aldo; Bellini, Stefania; Burnelli, Silvia; Granaiola, Massimiliano; Leoni, Alberto; Locatelli, Alessandra; Morigi, Rita; Rambaldi, Mirella; Varoli, Lucilla] Univ Bologna, Dipartimento Sci Farmaceut, I-40126 Bologna, Italy. [Calonghi, Natalia; Cappadone, Concettina; Zini, Maddalena; Stefanelli, Claudio; Masotti, Lanfranco] Univ Bologna, Dipartimento Biochim G Moruzzi, I-40126 Bologna, Italy. [Shoemaker, Robert H.] NCI, Screening Technol Branch, Dev Therapeut Program, Div Canc Treatment & Diag, Frederick, MD 21702 USA.;Andreani, A, Univ Bologna, Dipartimento Sci Farmaceut, Via Belmeloro 6, I-40126 Bologna, Italy.;aldo.andreani@unibo.it
    1. Year: 2010
    2. Date: Aug
  2. Journal: Journal of Medicinal Chemistry
    1. 53
    2. 15
    3. Pages: 5567-5575
  4. Type of Article: Article
  5. ISSN: 0022-2623
  1. Abstract:

    The synthesis of new substituted E-3-(3-indolylmethylene)-1,3-dihydroindo1-2-ones is reported. The antitumor activity was evaluated according to protocols available at the National Cancer Institute (NCI), Bethesda, MD. Structure activity relationships are discussed. The action of selected compounds was investigated in MCF-7 breast cancer cells. The ability of these derivatives to inhibit cellular proliferation was accompanied by increased level of p53 and its transcriptional targets p21 and Bax, interference in the cell cycle progression with cell accumulation in the G2/M phase, and activation of apoptosis.

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External Sources

  1. View Full Text
  2. DOI: 10.1021/jm1007165
  3. View record in Web of Science®
  4. WOS: 000280523300016

Library Notes

  1. Fiscal Year: FY2009-2010
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