Nineteen isosteviol derivatives were designed and synthesized by C-16, C-19 and D-ring modifications of isosteviol. These compounds were screened for their cytotoxic activities against Hela and A549 cells in vitro. Among them, the inhibitory effect of compounds 3b and 16 on Hela cells was comparable to that of the positive control gefitinib, and the compounds 3b (IC50=7.84 ± 0.84 μM) and 7a (IC50=6.89 ± 0.33 μM) exhibited significant cytotoxicity superior to gefitinib (IC50=11.02 ± 3.27 μM) against A549 cells.
Keywords: Synthesis; antiproliferative effects; isosteviol.