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Molecules 2012, 17(5), 4972-4985; doi:10.3390/molecules17054972
Article

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

1, 1, 2, 1, 1, 1, 1, 1 and 1,*
Received: 19 March 2012; in revised form: 18 April 2012 / Accepted: 20 April 2012 / Published: 30 April 2012
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Abstract: 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.
Keywords: angiogenesis; anti-tumor; combination principles; ligustrazine derivatives; low toxicity angiogenesis; anti-tumor; combination principles; ligustrazine derivatives; low toxicity
This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

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MDPI and ACS Style

Wang, P.; She, G.; Yang, Y.; Li, Q.; Zhang, H.; Liu, J.; Cao, Y.; Xu, X.; Lei, H. Synthesis and Biological Evaluation of New Ligustrazine Derivatives as Anti-Tumor Agents. Molecules 2012, 17, 4972-4985.

AMA Style

Wang P, She G, Yang Y, Li Q, Zhang H, Liu J, Cao Y, Xu X, Lei H. Synthesis and Biological Evaluation of New Ligustrazine Derivatives as Anti-Tumor Agents. Molecules. 2012; 17(5):4972-4985.

Chicago/Turabian Style

Wang, Penglong; She, Gaimei; Yang, Yanan; Li, Qiang; Zhang, Honggui; Liu, Jie; Cao, Yinqiu; Xu, Xin; Lei, Haimin. 2012. "Synthesis and Biological Evaluation of New Ligustrazine Derivatives as Anti-Tumor Agents." Molecules 17, no. 5: 4972-4985.



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