4.7 Article

Syntheses and evaluation of new acridone derivatives for selective binding of oncogene c-myc promoter i-motifs in gene transcriptional regulation

Journal

CHEMICAL COMMUNICATIONS
Volume 54, Issue 16, Pages 2036-2039

Publisher

ROYAL SOC CHEMISTRY
DOI: 10.1039/c8cc00328a

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Funding

  1. National Natural Science Foundation of China [21472252, 81330077]
  2. Natural Science Foundation of Guangdong Province [2017A030313089]

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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.

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