Abstract
A series of natural aristolactams and their analogues have been prepared and evaluated for antitumor activity against human cancer cells, including multi-drug resistant cell lines. Naturally occurring aristolactams, such as aristolactam BII (cepharanone B), aristolactam BIII, aristolactam FI (piperolactam A), N-methyl piperolactam A, and sauristolactam showed moderate antitumor activities in selected cell lines. However, several synthetic aristolactam derivatives exhibited potent antitumor activities against a broad array of cancer cell lines with GI(50) values in the submicromolar range.
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 / toxicity
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Aporphines / chemical synthesis
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Aporphines / chemistry
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Aporphines / toxicity
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Cell Line, Tumor
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Drug Screening Assays, Antitumor
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Heterocyclic Compounds, 4 or More Rings / chemical synthesis*
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Heterocyclic Compounds, 4 or More Rings / chemistry
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Heterocyclic Compounds, 4 or More Rings / toxicity
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Humans
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Lactams / chemical synthesis*
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Lactams / chemistry
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Lactams / toxicity
Substances
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Antineoplastic Agents
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Aporphines
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Heterocyclic Compounds, 4 or More Rings
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Lactams
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aporphine