摘要
3α-bromo-epipicropodophyllin was prepared and its inhibition activities against KB cells andL1210 leukemia cells in vitro are higher than those of VP-16, a widely used drug in clinic at present. This is the firsttime to introduce substitution at C-3 of ring-C in the work of modifying structure of podophyllotoxin. It can betransformed easily to 4β-hydroxy-2,3-ene-apopicropodophyllin under basic condition, so that, correspondingderivatives of 2,3-ene-apopicropodophyllin with substitution on carbon-4 could be synthesized. This compound canbe regarded not only as a leading compound to be modified because of its antitumor activities, but also as anintermediate for the structure transformation.