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.

A 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 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.