Three new nitroxyl labeled derivatives of podophyllotoxin (4) under ba
r-(6) under bar have been synthesized and evaluated for their antitumo
r activity in vitro. Compounds (4) under bar-(6) under bar showed sign
ificant inhibitory activity against human nasopharyngeal carcinoma KB,
lung cancer A549 and stomach carcinoma SGC-7901 cells, as well as mous
e leukemia L1210 and P388 cells. Compounds (4) under bar and (5) under
bar exhibited comparable or superior activity to clinically used etop
oside (VP-16,(2) under bar) in their inhibition of these cell lines.