Issue 82, 2017

Selective recognition of c-myc promoter G-quadruplex and down-regulation of oncogene c-myc transcription in human cancer cells by 3,8a-disubstituted indolizinone

Abstract

C-myc promoter G-quadruplex is a very important target for developing anti-cancer drugs. However, highly selective recognition of DNA c-myc G-quadruplex with parallel configuration is also a very challenging problem. Here, we showed a new type of N-containing alkaloid, 3,8a-disubstituted indolizinone, which adopted a distorted configuration. 6-Methyl-3-(naphthalen-2-yl)-8a-(4-methylpyridin-2-yl)-indolizinone could selectively recognize DNA c-myc G-quadruplex leading to an obvious fluorescence enhancement by 11-fold, and meanwhile the G-quadruplex can be stabilized up to 90 °C. Further, it could down-regulate the transcription of oncogene c-myc in both human non-small cell line (A549) and human laryngeal epithelial cell line (Hep-2).

Graphical abstract: Selective recognition of c-myc promoter G-quadruplex and down-regulation of oncogene c-myc transcription in human cancer cells by 3,8a-disubstituted indolizinone

Supplementary files

Article information

Article type
Paper
Submitted
05 Sep 2017
Accepted
02 Nov 2017
First published
08 Nov 2017
This article is Open Access
Creative Commons BY license

RSC Adv., 2017,7, 51965-51969

Selective recognition of c-myc promoter G-quadruplex and down-regulation of oncogene c-myc transcription in human cancer cells by 3,8a-disubstituted indolizinone

F. Yang, X. Sun, L. Wang, Q. Li, A. Guan, G. Shen and Y. Tang, RSC Adv., 2017, 7, 51965 DOI: 10.1039/C7RA09870G

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