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

RSC Advances
2017.0

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-(4methylpyridin- 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 degrees 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).

Knowledge Graph

Similar Paper

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
RSC Advances 2017.0
Selective recognition of DNA parallel G-quadruplexes by 3,8a-disubstituted indolizinones
Bioorganic & Medicinal Chemistry 2021.0
Discovery of a New Four-Leaf Clover-Like Ligand as a Potent c-MYC Transcription Inhibitor Specifically Targeting the Promoter G-Quadruplex
Journal of Medicinal Chemistry 2018.0
Design, Synthesis, and Evaluation of New Selective NM23-H2 Binders as c-MYC Transcription Inhibitors via Disruption of the NM23-H2/G-Quadruplex Interaction
Journal of Medicinal Chemistry 2017.0
Alkyne-substituted diminazene as G-quadruplex binders with anticancer activities
European Journal of Medicinal Chemistry 2016.0
New Disubstituted Quindoline Derivatives Inhibiting Burkitt’s Lymphoma Cell Proliferation by Impeding c-MYC Transcription
Journal of Medicinal Chemistry 2017.0
Discovery of Novel 11-Triazole Substituted Benzofuro[3,2-b]quinolone Derivatives as c-myc G-Quadruplex Specific Stabilizers via Click Chemistry
Journal of Medicinal Chemistry 2017.0
Design, Synthesis, and Evaluation of New Sugar-Substituted Imidazole Derivatives as Selective c-MYC Transcription Repressors Targeting the Promoter G-Quadruplex
Journal of Medicinal Chemistry 2022.0
New Dibenzoquinoxalines Inhibit Triple-Negative Breast Cancer Growth by Dual Targeting of Topoisomerase 1 and the c-MYC G-Quadruplex
Journal of Medicinal Chemistry 2021.0
Preferential stabilization of c-MYC and BCL-2 promoter G-quadruplexes by a natural betaine-type alkaloid
Phytochemistry Letters 2022.0