Fluorinated Modification of Neo-Tanshinlactone and Antiproliferative Activity Evaluation

Several neo-tanshinlactone derivatives with fluorine or the trifluoromethyl group were synthesized and their antiproliferative activities were evaluated. Compared with neo-tanshinlactone, fluorinated derivatives showed a broad activity spectrum against human tumor lines. For a neo-tanshinlactone chemical skeleton, these results also indicated that the hydrophobic group (methyl) at C-4 position and the carbon–carbon double bond of ring-D might play a crucial role in selective antibreast cancer activity. In addition, the synthesized compounds 10 and 17 showed a broad range of antiproliferative activity with IC50 values of 15–40 μM.