Synthesis of nordihydroguaiaretic acid derivatives and their bioactivities on S. pombe and K562 cell lines.

Abstract

Nordihydroguaiaretic acid (NDGA) and its synthetic analogues are potentially useful in treating diseases related to cancers, diabetes, viral and bacterial infections, and inflammation. In this paper, we report the optimal synthetic methods and the bioactivity study of terameprocol 2, NDGA derivative 3, and its cyclized analogue 4. The IC50 of these three compounds 2, 3 and 4 on the growth metabolism of Schizosacchromyces pombe and K562 cell lines were determined by microcalorimetry. The preliminary results showed that the compounds 2, 3 and 4 possessed good inhibition activities on S. pombe and K562 cell lines, and exhibited bidirectional biological effect and Hormesis effect. In particular, terameprocol 2 was found to possess the most potent inhibitory effect on K562 cell lines.

• Authors: Xu Li, Jian-Hong Jiang, Qingqi Chen, Sheng-Xiong Xiao, Chuan-Hua Li, Hui-Wen Gu, Hui Zhang, Ji-Lin Hu, Fei-Hong Yao, Qiang-Guo Li
• Journal: European journal of medicinal chemistry (Eur J Med Chem) Vol. 62 Pg. 605-13 (Apr 2013) ISSN: 1768-3254 [Electronic] France
• PMID: 23434529 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
• Copyright: Copyright © 2013 Elsevier Masson SAS. All rights reserved.

Chemical References

• Antifungal Agents
• Masoprocol

Topics

• Antifungal Agents (chemical synthesis, chemistry, pharmacology)
• Dose-Response Relationship, Drug
• Humans
• K562 Cells
• Masoprocol (chemical synthesis, chemistry, pharmacology)
• Microbial Sensitivity Tests
• Molecular Structure
• Schizosaccharomyces (drug effects)
• Structure-Activity Relationship
• Tumor Cells, Cultured