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Synthesis and Biological Evaluation of New Ligustrazine Derivatives as Anti-Tumor Agents

Author(s): Penglong Wang | Gaimei She | Yanan Yang | Qiang Li | Honggui Zhang | Jie Liu | Yinqiu Cao | Xin Xu | Haimin Lei

Journal: Molecules
ISSN 1420-3049

Volume: 17;
Issue: 5;
Start page: 4972;
Date: 2012;
Original page

Keywords: angiogenesis | anti-tumor | combination principles | ligustrazine derivatives | low toxicity

To discover new anti-cancer agents with multi-effect and low toxicity, a series of ligustrazine derivatives were synthesized using several effective anti-tumor ingredients of Shiquandabu Wan as starting materials. Our idea was enlightened by the “combination principle” in drug discovery. The ligustrazine derivatives’ anti-tumor activities were evaluated on the HCT-8, Bel-7402, BGC-823, A-549 and A2780 human cancer cell lines. In addition the angiogenesis activities were valued by the chick chorioallantoic membrane (CAM) assay. 1,7-bis(4-(3,5,6-Trimethylpyrazin-2-yl)-3-methoxyphenyl)-1,6-heptadiene-3,5-dione (4) and 3 α,12 α-dihydroxy-5β-dholanic acid-3,5,6-trimethylpyrazin-2-methyl ester (5) not only displayed antiproliferative activities on these cancer cells, but also dramatically suppressed normal angiogenesis in CAM. The LD50 value of the compound 5 exceeded 3.0 g/kg by oral administration in mice.
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