期刊
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
卷 53, 期 -, 页码 52-63出版社
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2012.03.034
关键词
c-myc G-Quadruplex; 5,6-Dihydrobenzo[c]acridine derivatives; Selectivity; 12-N-Methylation; Binding affinity
资金
- Natural Science Foundation of China [21172272]
- International S&T Cooperation Program of China [2010DFA34630]
- Science Foundation of Guangzhou [2009A1-E011-6]
12-N-Methylated and non-methylated 5,6-dihydrobenzo[c]acridine derivatives were designed and synthesized as new series of c-myc G-quadruplex binding ligands. Their interactions with c-myc G-quadruplex were evaluated using fluorescence resonance energy transfer (FRET) melting assay, circular dichroism (CD) spectroscopy, surface plasmon resonance (SPR), polymerase chain reaction (PCR) stop assay, and molecular modeling. Compared with the non-methylated derivatives, 12-N-methylated derivatives had stronger binding affinity and stabilizing ability to c-myc G-quadruplex structure, and could more effectively stack on the G-quartet surface. All these derivatives had high selectivity for c-myc G-quadruplex DNA over duplex DNA. The reverse transcription (RT) PCR assay showed that compound 21c could down-regulate transcription of c-myc gene in Ramos cell line containing NHE III1 element, but had no effect in CA46 cell line with NHE III1 element removed. (C) 2012 Elsevier Masson SAS. All rights reserved.
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