In our studies on the phytochemistry and biological activities of Croton tonkinensis Gagnep. (Euphorbiaceae) oriented by traditional medicine interesting biological activities of the plant were demonstrated in correlation with the ent-kaurane-type diterpenoid constituents. The high accumulation of the active principle ent-18-acetoxy-7 -hydroxykaur-16-en-15-one (1) led to our recent study on the chemical modification of this lead compound. In this paper the transformations of 1 into several derivatives by hydrolysis, acetylation, and oxydation were reported. The cytotoxic activity against of the transformation products Hep-G2 and LU cells was evaluated