Abstract
Two series of azanaphthoquinone annelated pyrrolo oximes have been synthesized. The antiproliferative activities of 10 compounds were evaluated on at least four different cell lines. One series of pyrrolo derivatives showed high cytotoxic activity. The effects on cell cycle and caspase activity were investigated. Compounds 9a and 9b showed an accumulation of cells in G2/M phase. Substantial and dose-dependent caspase activity was found after treatment of cells with 9a and 9b. This indicates an apoptosis inducing property of these compounds.
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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Caspases / drug effects
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Cell Cycle / drug effects
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Cell Line, Tumor
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Dose-Response Relationship, Drug
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Drug Screening Assays, Antitumor
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HeLa Cells
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Humans
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Mitoxantrone / analogs & derivatives
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Mitoxantrone / chemical synthesis*
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Mitoxantrone / pharmacology
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Molecular Structure
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Naphthoquinones / chemical synthesis*
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Naphthoquinones / chemistry
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Naphthoquinones / pharmacology
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Oximes / chemical synthesis*
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Oximes / chemistry
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Oximes / pharmacology
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Pyrroles / chemical synthesis*
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Pyrroles / chemistry
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Pyrroles / pharmacology
Substances
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Antineoplastic Agents
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Naphthoquinones
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Oximes
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Pyrroles
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Mitoxantrone
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Caspases