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Graphical abstract Highlights • A series of novel 25-OCH 3 -PPD derivatives were synthesized. • Cytotoxic activities of the derivatives were evaluated on five human tumor cell lines. • Compounds 3a , 14a and 18a exhibited strong anti-tumor activities. • Having aromatic ester at the C3 position could enhance the antiproliferative activities. Abstract Previously we have reported that 25-OCH 3 -PPD could suppress the reproduction of cancer cells and cause apoptosis without obvious toxicity. Herein, we aimed to enhance its bioactivity by introducing aromatic groups to its dammarane-type skeleton. These synthesized derivatives were tested for their inhibitory activities against five cancer cell lines. Of them, compounds 3a , 14a and 18a had the strongest antiproliferative activities against tumor cells (IC 50 < 15 µM, 5-fold to 10-fold increases than 25-OCH 3 -PPD). Especially compound 14a displayed the most potent activity against DU145, MCF-7 and HepG2 cells (IC 50 = 6.7 ± 0.8, 4.3 ± 0.8 and 5.8 ± 0.6 µM, respectively). Structure-activity relationships demonstrated that having aromatic ester at the C3 position could improve the bioactivity. The data provided new insights into exploring novel antiproliferative lead compounds. [ABSTRACT FROM AUTHOR]

In the current work, 12 novel 25-hydroxyprotopanaxadiol (25-OH-PPD) derivatives were synthesized by reacting with chloroacetyl chloride. And their in vitro antitumor activities were evaluated on six human tumor cell lines by MTT assay. The results demonstrated that, as compared with 25-OH-PPD, compounds 4 , 6 and 7 exhibited higher cytotoxic activity on all tested cell lines. Of them, compound 4 showed strongly inhibition against MCF-7, HCT-116 and Lovo cells with IC 50 values of 1.7, 1.6 and 2.1 μM, respectively. The IC 50 values of compound 6 against HCT-116 and 7 against MCF-7 were the lowest (1.2 and 1.6 μM, respectively). It was also noted that compound 4 showed a 20- to 100-fold greater growth inhibition than ginsenoside-Rg 3 (an anti-cancer regular drug in China). In conclusion, the data revealed that compounds 4 , 6 and 7 were potential candidates for anti-tumor treatment and may be useful for the development of novel antiproliferative agents. [ABSTRACT FROM AUTHOR]