Substituted E-3-(3-indolylmethylene)-1,3-dihydroindol-2-ones with antitumor activity. In depth study of the effect on growth of breast cancer cells

具有抗肿瘤活性的取代E-3-(3-吲哚亚甲基)-1,3-二氢吲哚-2-酮。深入研究对乳腺癌细胞生长的影响

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作者:Aldo Andreani, Stefania Bellini, Silvia Burnelli, Massimiliano Granaiola, Alberto Leoni, Alessandra Locatelli, Rita Morigi, Mirella Rambaldi, Lucilla Varoli, Natalia Calonghi, Concettina Cappadone, Maddalena Zini, Claudio Stefanelli, Lanfranco Masotti, Robert H Shoemaker

Abstract

The synthesis of new substituted E-3-(3-indolylmethylene)-1,3-dihydroindol-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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