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.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Antineoplastic Agents / chemical synthesis*
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Antineoplastic Agents / chemistry
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Antineoplastic Agents / pharmacology
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Apoptosis / drug effects
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Breast Neoplasms
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Cell Cycle / drug effects
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Cell Proliferation / drug effects
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Cyclin-Dependent Kinase Inhibitor p21 / metabolism
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Cytostatic Agents / chemical synthesis
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Cytostatic Agents / chemistry
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Cytostatic Agents / pharmacology
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Cytotoxins / chemical synthesis
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Cytotoxins / chemistry
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Cytotoxins / pharmacology
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Drug Screening Assays, Antitumor
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Female
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Humans
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Indoles / chemical synthesis*
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Indoles / chemistry
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Indoles / pharmacology
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Stereoisomerism
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Structure-Activity Relationship
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Tumor Suppressor Protein p53 / metabolism
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bcl-2-Associated X Protein / metabolism
Substances
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Antineoplastic Agents
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Cyclin-Dependent Kinase Inhibitor p21
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Cytostatic Agents
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Cytotoxins
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Indoles
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Tumor Suppressor Protein p53
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bcl-2-Associated X Protein