Citation: Wen Li Xi, Qian Cai, Yan Bo Tang, Hua Sun, Zhi Yan Xiao. Design and synthesis of novel cytotoxic podophyllotoxin derivatives[J]. Chinese Chemical Letters, ;2010, 21(10): 1153-1156. doi: 10.1016/j.cclet.2010.03.040 shu

Design and synthesis of novel cytotoxic podophyllotoxin derivatives

Wen Li Xi ^a, ,
Qian Cai ^a ,
Yan Bo Tang ^b ,
Hua Sun ^b ,
Zhi Yan Xiao ^b

a School of Pharmacy, Liaoning University of Traditional Chinese Medicine, Dalian 116600, China;
b Key Laboratory of Bioactive Substances and Resources Utilization of Chinese Herbal Medicine, Ministry of Education & Institute of MateriaMedica, Chinese Academy of Medical Sciences & Peking Union Medical College, Beijing 100050, China

Received Date: 25 January 2010

In order to investigate the effect of different C4 linkage moieties on the cytotoxicity of podophyllotoxin derivatives, novel 4-N-and 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 IC₅₀ value at 10^-7 mol/L level.
- Podophyllotoxin,
- C4-derivation,
- Cytotoxicity
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