2. Academic Validation
  3. Synthesis of nordihydroguaiaretic acid derivatives and their bioactivities on S. pombe and K562 cell lines

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

  • Eur J Med Chem. 2013 Apr:62:605-13. doi: 10.1016/j.ejmech.2013.01.028.
Xu Li 1,  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
Affiliations

Affiliation

  • 1 Hunan Provincial Key Laboratory of Xiangnan Rare-Precious Metals Compounds and Applications, Department of Chemistry and Life Science, Xiangnan University, Chenzhou 423000, Hunan Province, PR China.
PMID: 23434529 DOI: 10.1016/j.ejmech.2013.01.028
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.

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