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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,*
1 School of Chinese Pharmacy, Beijing University of Chinese Medicine, Beijing 100102, China 2 Institute of Materia Medica, Chinese Academy of Medical Sciences Peking Union Medical College, Beijing 100050, China
* Author to whom correspondence should be addressed.
Received: 19 March 2012 / Revised: 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 (CC BY 3.0).

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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.

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