Abstract
A series of cycloberberine derivatives were designed, synthesized and evaluated for their anti-cancer activities in vitro. Among these analogs, compounds 6c, 6e and 6g showed strong inhibition on human HepG2 cells. They afforded a potent effect against DOX-resistant MCF-7 breast cells as well. The primary mechanism showed that cell cycle was blocked at G2/M phase of HepG2 cells treated with 6g using flow cytometry assay. It significantly inhibited the activity of DNA Top I at the concentration of 0.1 mg mL-1. Our results provided a basis for the development of this kind of compounds as novel anti-cancer agents.
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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Berberine / analogs & derivatives*
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Berberine / chemical synthesis*
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Berberine / chemistry
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Berberine / pharmacology
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Cell Cycle / drug effects
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Cell Proliferation / drug effects
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DNA Topoisomerases, Type I / metabolism
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Doxorubicin / pharmacology
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Drug Resistance, Neoplasm
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Hep G2 Cells
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Humans
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MCF-7 Cells
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Molecular Structure
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Structure-Activity Relationship
Substances
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Antineoplastic Agents
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Berberine
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Doxorubicin
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DNA Topoisomerases, Type I