Abstract
2-Piperazinyl naphthoquinones (2) and 2-piperidinyl naphthoquinones (3) were designed and synthesized as new cytotoxic and apoptosis inducing agents by utilizing the anti-parasite drug atovaquone as lead compound. Several compounds displayed significantly improved cytotoxic activities against a panel of cancer cell lines than that of atovaquone. These compounds also induced apoptosis through activating pro-apoptotic caspases 9 and 3.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Anti-Infective Agents / chemistry
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Anti-Infective Agents / pharmacology
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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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Apoptosis*
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Atovaquone / analogs & derivatives*
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Atovaquone / chemistry
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Atovaquone / pharmacology
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Caspase 3 / metabolism
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Caspase 9 / metabolism
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Cell Line, Tumor
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Crystallography, X-Ray
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Drug Design
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Drug Screening Assays, Antitumor
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Humans
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Male
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Molecular Conformation
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Naphthoquinones / chemical synthesis
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Naphthoquinones / chemistry*
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Naphthoquinones / toxicity
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Prostatic Neoplasms / drug therapy
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Prostatic Neoplasms / pathology
Substances
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Anti-Infective Agents
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Antineoplastic Agents
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Naphthoquinones
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Caspase 3
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Caspase 9
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Atovaquone