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

被引：19

作者：

Andreani, Aldo ^{[1
]}

Bellini, Stefania ^{[1
]}

Burnelli, Silvia ^{[1
]}

Granaiola, Massimiliano ^{[1
]}

Leoni, Alberto ^{[1
]}

Locatelli, Alessandra ^{[1
]}

Morigi, Rita ^{[1
]}

Rambaldi, Mirella ^{[1
]}

Varoli, Lucilla ^{[1
]}

Calonghi, Natalia ^{[2
]}

Cappadone, Concettina ^{[2
]}

Zini, Maddalena ^{[2
]}

Stefanelli, Claudio ^{[2
]}

Masotti, Lanfranco ^{[2
]}

Shoemaker, Robert H. ^{[3
]}

机构：

[1] Univ Bologna, Dipartimento Sci Farmaceut, I-40126 Bologna, Italy

[2] Univ Bologna, Dipartimento Biochim G Moruzzi, I-40126 Bologna, Italy

[3] NCI, Screening Technol Branch, Dev Therapeut Program, Div Canc Treatment & Diag, Frederick, MD 21702 USA

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 2010年 / 53卷 / 15期

关键词：

POTENTIAL COANTHRACYCLINIC ACTIVITY; MITOMYCIN ANTIBIOTICS; DERIVATIVES; DEATH; APOPTOSIS; CASPASES; KINASES; PATHWAY; P53;

D O I：

10.1021/jm1007165

中图分类号：

R914 [药物化学];

学科分类号：

100705 [微生物与生化药学];

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.

引用

页码：5567 / 5575

页数：9

共 38 条

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p21 in cancer: intricate networks and multiple activities [J].