Diterpenenes were widely found in Zingiberaceae family,and some of them showed various bioactivities.Our previous researches on Hedychium genus resulted in obtaining series of diterpenes with significant cytotoxic or antitumor activities.Three butenolide diterpene derivatives 4,5,and 7 were synthesized from three Zingiberaceae diterpenes,coronarin E (1),hedychenone (2) and yunnancoronarin A (3),respectively.Compound 1 underwent photooxygenation reaction in CH₂Cl₂ to obtain 4,in which tetraphenyl porphyrin was served as photosensitizer and in the presence of N,N-diisopropylethylamine.Similarly,Compound 2 underwent photooxygenation to get 5.Compound 3 was benzoylated to obtain 6,which was further photooxygenated to get 7.Compounds 1,2,5,6 and 7 were subjected to in vitro cytotoxicity bioassays,the result indicates that compounds 5 and 7 have significant cytotoxicity against five tumor cell lines,including human liver cancer cells SMMC-7721,human lung cancer cells A-549,human breast cancer cells MCF-7,human colon cancer cells SW480 and human leukemia cells HL-60,and their inhibitory activities against SMMC-7721,A-549,MCF-7 and SW480 cell lines were higher than that of cisplatin (positive control).Compounds 4,5 and 7 were tested for in vivo antitumor activity in mice.As a result,the three compounds showed significant inhibitory effect on H22 and S₁₈₀ tumor in mice.Compounds 4 had the strongest inhibitory effect,and its inhibitory rate on H22 was 47.44%,which was close to that of ifosfamide (positive control).Inhibitory rates of 4 and 7 on S180 were 60.16% and 45.20%,which were higher than that of ifosfamide.