9-N-Substituted berberine derivatives: stabilization of G-quadruplex DNA and down-regulation of oncogene c-myc.

@article{Ma20089NSubstitutedBD,
  title={9-N-Substituted berberine derivatives: stabilization of G-quadruplex DNA and down-regulation of oncogene c-myc.},
  author={Yan Ma and Tian-Miao Ou and Jin-Qiang Hou and Yu-jing Lu and Jia-Heng Tan and Lian-Quan Gu and Zhi-Shu Huang},
  journal={Bioorganic & medicinal chemistry},
  year={2008},
  volume={16 16},
  pages={7582-91}
}
A series of 9-N-substituted berberine derivatives (2a-j) were synthesized and evaluated as a new class of G-quadruplex binding ligands. G-quadruplex of DNA had been proven to be the transcription controller of human c-myc gene. The interaction of 9-N-substituted berberine derivatives with G-quadruplex DNA in c-myc was examined via EMSA, CD spectroscopy, FRET-melting method, PCR-stop assay, competitive dialysis, cell proliferation assay, and RT-PCR assay. The experiment results indicated that… CONTINUE READING

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