Next Article in Journal
Bioassay-Guided Antidiabetic Study of Phaleria macrocarpa Fruit Extract
Previous Article in Journal
Synthesis and Antimicrobial Evaluation of Some Pyrazole Derivatives
Article Menu

Article Versions

Export Article

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

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

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
Download PDF [403 KB, uploaded 18 June 2014]

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).

Supplementary material

Scifeed alert for new publications

Never miss any articles matching your research from any publisher
  • Get alerts for new papers matching your research
  • Find out the new papers from selected authors
  • Updated daily for 49'000+ journals and 6000+ publishers
  • Define your Scifeed now

SciFeed Share & Cite This Article

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.

Show more citation formats Show less citations formats

Related Articles

Article Metrics

Article Access Statistics

1

Comments

[Return to top]

Molecules EISSN 1420-3049 Published by MDPI AG, Basel, Switzerland RSS E-Mail Table of Contents Alert
Back to Top