LAUSR

HIGHLIGHTS25 novel protopanaxadiol analogs have been synthesized.Combine with non‐protein amino acids moiety exhibited anti‐canceractivities.Compounds 9 and 14 exhibited strong biological activity on cancer celllines. ABSTRACT As active components of ginseng, 25‐methoxylprotopanaxadiol and 25‐hydroxyprotopanaxadiol exhibited an ability to inhibit the growth and proliferation or to induce the differentiation and apoptosis of tumour cells. We modified 25‐OCH3‐PPD and 25‐OH‐PPD with non‐protein amino acids and a series of derivatives was obtained by chromatographic separation, purification and spectroscopy analysis. Thirteen derivatives of 25‐OCH3‐PPD (compounds 1–13) and 12 derivatives of 25‐OH‐PPD (compounds 14–25) were synthesised. The anti‐cancer activities of the derivatives were evaluated on HCT‐116 and BGC‐823 cell lines by MTT assay. Compound 9 and compound 14 exhibited considerable anti‐tumour activity for HCT‐116 and BGC‐823 cell lines, exhibited higher cytotoxic activity than 25‐OCH3‐PPD and 25‐OH‐PPD. Therefore, these ginsenoside derivatives could be used as potential lead for the development of a new type of anticancer agent.