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Synthesis and structure-activity relationship of cycloberberine as anti-cancer agent

Bi, C.-W.; Zhang, C.-X.; Li, Y.-B.; Zhao, W.-L.; Shao, R.-G.; Mei, L.; Song, D.-Q.

Yao Xue Xue Bao 48(12): 1800-1806

2013

ISSN/ISBN: 0513-4870
PMID: 24689237
Document Number: 666486
A series of cycloberberine derivatives were designed, synthesized and evaluated for their anti-cancer activities in vitro. Among these analogs, compounds 6c, 6e and 6g showed strong inhibition on human HepG2 cells. They afforded a potent effect against DOX-resistant MCF-7 breast cells as well. The primary mechanism showed that cell cycle was blocked at G2/M phase of HepG2 cells treated with 6g using flow cytometry assay. It significantly inhibited the activity of DNA Top I at the concentration of 0.1 mg mL-1. Our results provided a basis for the development of this kind of compounds as novel anti-cancer agents.

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