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

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 tra...

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Veröffentlicht in:Chemical communications (Cambridge, England) England), 2018, Vol.54 (16), p.2036-2039
Hauptverfasser: Shu, Bing, Cao, Jiaojiao, Kuang, Guotao, Qiu, Jun, Zhang, Meiling, Zhang, Yan, Wang, Mingxue, Li, Xiaoya, Kang, Shuangshuang, Ou, Tian-Miao, Tan, Jia-Heng, Huang, Zhi-Shu, Li, Ding
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Sprache:eng
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Zusammenfassung: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.
ISSN:1359-7345
1364-548X
DOI:10.1039/c8cc00328a