Structure-based design of flavone derivatives as c-myc oncogene down-regulators. Yang, H., Zhong, H., Leung, K., Chan, D. S., Ma, V. P., Fu, W., Nanjunda, R., Wilson, W D., Ma, D., & Leung, C. European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences, 48(1-2):130–41, January, 2013. Publisher: Elsevier B.V.![Structure-based design of flavone derivatives as c-myc oncogene down-regulators. [link]](https://bibbase.org/img/filetypes/link.svg "link")
Paper doi abstract bibtex Based on molecular docking analysis of complexes between flavone and the c-myc G-quadruplex, we designed and screened 30 flavone derivatives containing various side chains that could potentially form interactions with the G-quadruplex grooves. As a proof-of-concept, the highest-scoring flavone derivatives containing cationic pyridinium side chains were synthesized and their interactions with the c-myc G-quadruplex were examined using a PCR-stop assay. The stabilizing effects of the flavone derivatives were found to be selective towards the c-myc G-quadruplex over other biologically relevant G-quadruplex structures, such as the human telomeric sequence (HTS). The interaction between the most potent compound of the series and the c-myc G-quadruplex was examined in depth using UV-Vis titration, molecular modeling and CD spectroscopy. Our results suggest that in addition to stabilizing the c-myc G-quadruplex, the flavone derivatives were capable of inducing the formation of the G-quadruplex structure even in the absence of monovalent cations. The flavone derivatives were found to be potent inhibitors of c-myc promoters within the cellular environment and displayed promising cytotoxic behavior against human cancer cell lines.
@article{Yang2013,
title = {Structure-based design of flavone derivatives as c-myc oncogene down-regulators.},
volume = {48},
issn = {1879-0720},
url = {http://www.ncbi.nlm.nih.gov/pubmed/23127826},
doi = {10.1016/j.ejps.2012.10.010},
abstract = {Based on molecular docking analysis of complexes between flavone and the c-myc G-quadruplex, we designed and screened 30 flavone derivatives containing various side chains that could potentially form interactions with the G-quadruplex grooves. As a proof-of-concept, the highest-scoring flavone derivatives containing cationic pyridinium side chains were synthesized and their interactions with the c-myc G-quadruplex were examined using a PCR-stop assay. The stabilizing effects of the flavone derivatives were found to be selective towards the c-myc G-quadruplex over other biologically relevant G-quadruplex structures, such as the human telomeric sequence (HTS). The interaction between the most potent compound of the series and the c-myc G-quadruplex was examined in depth using UV-Vis titration, molecular modeling and CD spectroscopy. Our results suggest that in addition to stabilizing the c-myc G-quadruplex, the flavone derivatives were capable of inducing the formation of the G-quadruplex structure even in the absence of monovalent cations. The flavone derivatives were found to be potent inhibitors of c-myc promoters within the cellular environment and displayed promising cytotoxic behavior against human cancer cell lines.},
number = {1-2},
journal = {European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences},
author = {Yang, Hui and Zhong, Hai-Jing and Leung, Ka-Ho and Chan, Daniel Shiu-Hin and Ma, Victor Pui-Yan and Fu, Wai-Chung and Nanjunda, Rupesh and Wilson, W David and Ma, Dik-Lung and Leung, Chung-Hang},
month = jan,
year = {2013},
pmid = {23127826},
note = {Publisher: Elsevier B.V.},
keywords = {\#nosource},
pages = {130--41},
}
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