Abstract
We synthesized a series of acridone derivatives for specific binding ligands of i-motifs. Subsequent evaluations showed that B19 could selectively bind to and stabilize the c-myc promoter i-motif without significant binding to the G-quadruplex and duplex DNA. This caused down-regulation of c-myc transcription and expression, resulting in tumor cell apoptosis.
MeSH terms
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Acridones / chemical synthesis
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Acridones / chemistry
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Acridones / pharmacology*
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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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Binding Sites / drug effects
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Cell Line, Tumor
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Cell Proliferation / drug effects
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Dose-Response Relationship, Drug
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Down-Regulation / drug effects
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Down-Regulation / genetics
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Drug Screening Assays, Antitumor
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Fluorescence Resonance Energy Transfer
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Gene Expression Regulation, Neoplastic / drug effects*
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Gene Expression Regulation, Neoplastic / genetics
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Humans
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Molecular Structure
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Promoter Regions, Genetic / genetics*
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Proto-Oncogene Proteins c-myc / genetics*
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Structure-Activity Relationship
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Transcription, Genetic / drug effects*
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Transcription, Genetic / genetics
Substances
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Acridones
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Antineoplastic Agents
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Proto-Oncogene Proteins c-myc
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acridone