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

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.

Three compounds of NDGA derivatives were synthesized and their bioactivities were determined by microcalorimetry. The preliminary results indicated that terameprocol 2 might be valuable source for potent anticancer drug candidates.Figure optionsDownload as PowerPoint slideHighlights
► Three NDGA derivatives were optimized synthesized and characterized.
► Bioactivities of the compounds on S. pombe and K562 cells were determined by microcalorimetry.
► The synthetic compounds showed good inhibition activities on S. pombe and K562 cells.
► Terameprocol 2 was found to possess the most potent inhibitory effect on K562 cell lines.