Semi-synthesis and anti-tumor evaluation of novel 25-hydroxyprotopanaxadiol derivatives

30 novel compounds have been synthesized from 25-hydroxyprotopanaxadiol (25-OH–PPD) and their in vitro anti-tumor activities were tested on three cancer cell lines and one normal cell line (IOSE144) by standard MTT assay. The results showed that compound 27 exhibited the best anti-tumor activity in the in vitro assays. Compounds 1, 2, 16, 17, 18, 27, 28 and 29 have better anti-tumor activities against MCF-7 and A549 cancer cell lines than 25–OH–PPD, together with low toxicity in the normal cell. The results may provide useful data for researching and developing new antitumor agents.

Graphical abstractA series of 25-OH–PPD derivatives have been synthesized and their antitumor activities were evaluated against a panel of human tumor cell lines and one normal cell by the standard MTT assay.Figure optionsDownload full-size imageDownload as PowerPoint slideHighlights► A series of 25-OH–PPD derivatives have been synthesized by simple acylation. ► Some compounds showed stronger antitumor activities than that of 5-Fu in vitro. ► The antitumor activities were affected by hydroxyl substitutions at C3 and C12.