Disclosed are a 4β-amino substituted podophyllotoxin derivative and a synthesis method therefor and the use thereof. The present invention respectively introduces the aromatic heterocyclic compounds anthraquinone, quinazoline, quinoline, indole, indazole, pyrimidine as substituent groups to position-4 of the C ring in the podophyllotoxin or 4′；-demethylepipodophyllotoxin to obtain the podophyllotoxin derivatives as shown in formula (V). Experiments involving in vitro tumour cell activity inhibition show that the antitumour activity of most of the compounds as shown in formula (V) of the present invention is significantly improved compared to that of the patented medicine of podophyllotoxin-“etoposide”.
