The present invention discloses an anilino-substituted podophyllin derivative having antitumor activity, method for preparation thereof, and use thereof. By means of anilino reactions, the present invention introduces 4-chloro-3-methylaniline, 3-fluoro-4-methoxyaniline, 4,4′-diaminodiphenylmethane, o-anisidine, 4-chloro-2-aminoanisole, anthranilonitrile, 2,6-dichloro-4-aminophenol, N,N-dimethylamino meta-aniline, 2-ethyl-5-nitroaniline, 2 2′-diaminodiphenylsulfide, or 2-aminobenzotrifluoride into position 4 of the active C-ring of podophyllotoxin or 4′-demethylepipodophyllotoxin to obtain the aniline-substituted podophyllotoxin derivative shown in formula (V) by means of multi-pathway and multi-target effects on tumor cells, said derivative has significantly increased antitumor activity, and can be prepared as an antineoplastic drug and applied in clinical antitumor therapy.
