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

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.