Design and synthesis of novel cytotoxic podophyllotoxin derivatives

• 出 处: Chinese Chemical Letters
• 发表日期: 2010年10期
• 关键词: cytotoxic linkage potent antitumor substituted highlights ongoing lignan condens

In order to investigate the effect of different C4 linkage moieties on the cytotoxicity of podophyllotoxin derivatives,novel 4-Nand 4-C-substituted 4’-O-demethylepipodophyllotoxin derivatives were designed and synthesized.All the compounds were tested against A549 and MCF-7 tumor cells in vitro,and six compounds showed significant cytotoxicity.The most active compound 9f was superior to GL-331,and exhibited potent cytotoxicity with IC_(50) value at 10~(-7) mol/L level.

In order to investigate the effect of different C4 linkage moieties on the cytotoxicity of podophyllotoxin derivatives, novel 4-Nand 4-C-substituted 4’-O-demethylepipodophyllotoxin derivatives were designed and synthesized. All the compounds were tested against A549 and MCF-7 tumor cells in vitro, and six compounds showed significant cytotoxicity. Most active compound 9f was superior to GL-331, and showed potent cytotoxicity with IC 50 value at 10 -7 mol / L level.