[Synthesis and antitumor activity of 4-O-(halogenated) acyl-4'-demethylepipodophyllotoxin analogues]

A series of 4-(halogenated)acyl-4'-demethylepipodophyllotoxin analogues were conveniently synthesized by selective esterification in the presence of BF3.Et2O, and screened in vitro against L1210 leukemia and KB cells. Most of these compounds showed marked antitumor activity and exhibited more potent activity than that of etoposide.