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.
A. Andreani, S. Bellini, S. Burnelli, M. Granaiola, A. Leoni, A. Locatelli, et al. (2010). 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. JOURNAL OF MEDICINAL CHEMISTRY, 53, 5567-5575 [10.1021/jm1007165].
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
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;
2010
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.I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
