Synthesis and Biological Evaluation of New Ligustrazine Derivatives As Anti-tumor Agents

Overview

Journal Molecules

Publisher MDPI

Specialty Biology

Date 2012 May 2

PMID 22547319

Citations 30

Authors

Penglong Wang

Gaimei She

Yanan Yang

Qiang Li

Honggui Zhang

Jie Liu

Yinqiu Cao

Xin Xu

Haimin Lei

Affiliations

Soon will be listed here.

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.

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