Abstract: Novel hybrid compounds 7a-7p were designed and synthesized via conjugating farnesylthiosalicylic acid(FTS)and hydroxylcinnamic acids, and their in vitro biological activities were evaluated. It was found that most compounds displayed good to moderate in vitro antitumor activities against six human cancer cells. Especially, the antitumor activities of compound 7b , with the IC₅₀ values of 5. 51-9. 25 μmol/L range against all tested cancer cells, were superior to those of FTS and sorafenib, and compound 7b could selectively inhibit the proliferation of tumor cells but not that of human normal cell. Furthermore, compound 7b significantly induced SMMC-7721 cell apoptosis in a dose-dependent manner.