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In current study,derivatives of 25-hydroxyprotopanaxadiol (25-OH-PPD) were prepared and their in vitro anti-tumor activities were tested on six different human tumor cell lines by standard MTT assay.The results showed combining an ester group combined with the presence of an amino acid moiety led to a 10-fold improved antitumor activity.Compound 1e exhibited the best anti-tumor activity in the in vitro assays.Compounds 2c,3c,4c,5c,6c and 8b showed better anti-tumor activities compared to the parent compound 25-OH-PPD.The current results may provide useful data for researching and developing new anti-cancer agents.