Abstract: 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.

Abstract: The present invention discloses a sulfur-substituted podophyllotoxin derivative, synthesis method thereof, and use thereof. The present invention introduces a rigid aromatic heterocyclic compound, as well as a further sulfonamidated product of 3-amino-5-mercapto-1,2,4-triazole, 2-amino-5-mercapto-1,3,4-thiadiazole, 4-methylbenzenesulfonyl chloride, or 4-methoxybenzenesulfonyl chloride as a substituent group, into position 4 of the C-ring of podophyllotoxin or 4?-demethylepipodophyllotoxin to obtain the podophyllotoxin derivative shown in formula (V), said derivative having significantly increased antitumor activity and reduced toxic side effects. Experiments on in vitro tumor cell inhibition indicate that the antitumor activity of the compound of formula (V) of the present invention is significantly higher than the antitumor activity of podophyllotoxin or 4?-demethylepipodophyllotoxin.

Abstract: A 4?-demethylepipodophyllotoxin derivative of formula (III) having anti-tumor activity is provided. After the activation of hydroxyl in position C4 of 4?-demethylepipodophyllotoxin, tetramethylpyrazine is introduced by transamination to obtain the 4?-demethylepipodophyllotoxin derivative which is preferably used to inhibit gastric cancer line BGC-823.

Abstract: A 4?-demethylepipodophyllotoxin derivative of formula(III) having anti-tumor activity is provided. After the activation of hydroxyl in position C4 of 4?-demethylepipodophyllotoxin, tetramethylpyrazine is introduced by transamination to obtain the 4?-demethylepipodophyllotoxin derivative which is preferably used to inhibit gastric cancer line BGC-823.

Abstract: A 4?-demethylepipodophyllotoxin derivative of formula(III) having anti-tumor activity is provided. After the activation of hydroxyl in position C4 of 4?-demethylepipodophyllotoxin, tetramethylpyrazine is introduced by transamination to obtain the 4?-demethylepipodophyllotoxin derivative which is preferably used to inhibit gastric cancer line BGC-823.

Abstract: A 4?-demethylepipodophyllotoxin derivative of formula(III) having anti-tumor activity is provided. After the activation of hydroxyl in position C4 of 4?-demethylepipodophyllotoxin, tetramethylpyrazine is introduced by transamination to obtain the 4?-demethylepipodophyllotoxin derivative which is preferably used to inhibit gastric cancer line BGC-823.