Synthesis of podophyllotoxin derivatives and their antitumor activity in vitro

Aim To find compounds with superior antitumor bioactivity and overcoming multidrug resistance.Methods Seven derivatives of podophyllotoxin were synthesized by linking 4β-amino-4-deoxypodophyllotoxin with alcohols through succinic acid.Their structures were confirmed by 1H-NMR,TOF-MS.Their antitumor activity was tested by MTT method against K562 and K562/AO2 in vitro.Results Seven derivatives were not reported by previous literature.The derivatives 5b,5d exhibit superior anticancer activity compared to VP-16 against K562 in vitro.The derivatives 5b,5c,5d and 5e may overcome MDR compared to VP-16 against K562/AO2 in vitro.Conclusion The results indicate that these compounds show high antitumor activity.