SYNTHESIS AND ANTITUMOR ACTIVITIES OF 4β-S-(5″-ALKYL-4″-AMINO-1″,2″,4″-TRIAZOLE-3″-YL)-4-DEOXY-4′-O-DEMETHYL-EPIPODOPHYLLOTOXIN DERIVATIVES

AIM: In order to search for podophyllotoxin analogue agents with fewer side effects and improved activity, the podophyllotoxin derivatives are to be synthesized. METHODS: Eight 4′-demethyl-podophyllotoxin analogues with 4β-S-triazoles have been synthesized from 4′-demethyl-podophyllotoxin. RESULTS: Eight 4′-demethyl-podophyllotoxin derivatives possessing 4β-S-triazoles have been synthesized and their antitumor activities were screened in vitro against HL-60, BGC-823, BcaP, KB and K₅₆₂ cells. CONCLUSION: The results indicated that these compounds showed high biological activity only towards K₅₆₂ cells.