Journal
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Volume 46, Issue 5, Pages 1906-1913Publisher
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2011.02.020
Keywords
Synthesis; Berberine; Quinolino-benzo-[5,6]-dihydroisoquindolium compounds; Biophysical and biochemical evaluation; C-myc G-quadruplex
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Funding
- Natural Science Foundation of China [U0832005, 90813011, 30801436]
- Ministry of Education of the People's Republic of China [200805581163]
- Guangdong Natural Science Foundation [8451008901000214]
- Science Foundation of Guangzhou [2009A1-E011-6]
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A series of quinolino-benzo-[5, 6]-dihydroisoquindolium compounds (3a, 3f, 3g, and 3j) derived from alkaloid berberine were designed and synthesized as novel G-quadruplex ligands. Subsequent biophysical and biochemical evaluation demonstrated that the addition of pyridine ring and amino group into berberine improved the binding ability and selectivity towards G-quadruplex DNA in comparison with the previously reported 9-N-substituted berberine derivatives. Furthermore, qRT-PCR assay showed compound 3j led the down-regulation of c-myc gene transcription in leukemia cell line HL60, while little effect on normal cell line ECV-304, which was consistent with the behavior of an effective G-quadruplex ligand targeting c-myc oncogene. (C) 2011 Elsevier Masson SAS. All rights reserved.
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