Objective A diterpeneoid， 7-hydroxyl-hedychenone was utilized to synthesis bioactive derivatives. Methods 7-hydroxyl-hedychenone was acylated or alkylated， as a result， four derivatives were obtained， three of which were subjected to in vitro antitumor bioassays. Results Four diterpene derivatives were obtained， one derivative showed antitumor activity against two cancer cell lines. Conclusion It is feasible to obtain derivatives with antitumor activity from natural diterpenoids.