Synthesis and antitumor activity of novel podophyllotoxin derivatives against multidrug-resistant cancer cells.

Seven novel 4β-N-substituted podophyllotoxin derivatives with indole rings were prepared and evaluated for cytotoxicity against human cancer cell lines HeLa, KB, KBV, K562, and K562/AO2. Most of them demonstrated improved antitumor activity and weak multidrug resistance compared to the drugs currently available.