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Synthesis and Biological Evaluation of New Ligustrazine Derivatives as Anti-Tumor Agents
School of Chinese Pharmacy, Beijing University of Chinese Medicine, Beijing 100102, China
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; in revised form: 18 April 2012 / Accepted: 20 April 2012 / Published: 30 April 2012
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
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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.
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.
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.