[Synthesis and antitumor activities of 4-acylthiol-4-deoxy-4'-demethylepipodophyllotoxin analogues]

This paper describes the synthesis and antitumor activity of 4-acylthiol-4-deoxy-4'-demethylepipodophyllotoxin analogues. 4-Mercapto-4-deoxy-4'-demethylepipodophyllotoxin prepared from 4'-demethylepipodophyllo-toxin with H2S in the presence of BF3.Et2O, was acylated with different acids using diethyl cyanophosphonate and thus, corresponding 4-acylthiol-4-deoxy-4'-demethyl epipodophyllotoxin analogues were synthesized. These compounds were screened in L1210 leukemia and KB cells, and one compound has activity similar to etoposide, and others were generally weaker than etoposide and corresponding 4-acylamido-4-deoxy-4'-demethylepipodophyllotoxin analogues.