The cytotoxicity and the cell-cycle action of altholactone (1), goniofufuro
ne (2), and eight altholactone derivatives. (5-12), were determined in vitr
o on L-1210 cells. Semisyntheses and structure-activity relationships of th
ese compounds are described. The results of this study suggest that the cyt
otoxicity of altholactone (1), 11-nitro-altholactone (8), and 7-chloro-6,7-
dihydroaltholactone (10) is due to the accumulation of the cells in the G2
+ M phase of the cell cycle.