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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

  作者 ANDREANI ALDO; BELLINI STEFANIA; BURNELLI SILVIA; GRANAIOLA MASSIMILIANO; LEONI ALBERTO; LOCATELLI ALESSANDRA; MORIGI RITA; RAMBALDI MIRELLA; VAROLI LUCILLA; CALONGHI NATALIA; CAPPADONE CONCETTINA; ZINI MADDALENA; STEFANELLI CLAUDIO; MASOTTI LANFRANCO; SHOEMAKER ROBERT H  
  选自 期刊  Journal of Medicinal Chemistry;  卷期  2010年53-15;  页码  5567-5575  
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[摘要]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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