Antiproliferative Activity of the Diterpenes Jatrophone and Jatropholone and Their Derivatives

The anti proliferative activity of the diterpenes jatropholone A and B, 16 semi-synthetic derivatives thereof, and that of jatrophone and its three derivatives was assessed on human cell cultures. The cells used comprised normal lung fibroblasts (MRC-5), gastric adenocarcinoma (AGS), leukemia (HL-60), lung cancer (SK-MES-1), and bladder carcinoma (J82). jatropholone A (1) was inactive against all the tumor cell lines; however, its acetylation rendered a compound with anti proliferative activity. The epimeric jatropholone B (8) was active against all the cancer cell lines, and its derivatives presented different effects on the selected cell lines. While jatrophone (19) showed strong anticancer activity, its derivatives 9 beta,13 alpha-dihydroxyisabellione and 13 alpha-hydroxy-9 beta-acetoxyisabellione were less active.