Design and synthesis of novel cytotoxic podophyllotoxin derivatives |
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| Authors: | Wen Li Xi Qian Cai Yan Bo Tang Hua Sun Zhi Yan Xiao |
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| Affiliation: | 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 |
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| Abstract: | 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 10-7M level. |
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| Keywords: | Podophyllotoxin C4-derivation Cytotoxicity |
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