Citation:
Kun Fang, Guo-Qiang Dong, Hai Gong, Na Liu, Zhen-Gang Li, Shi-Ping Zhu, Zhen-Yuan Miao, Jian-Zhong Yao, Wan-Nian Zhang, Chun-Quan Sheng. Design, synthesis and biological evaluation of E-ring modifi ed evodiamine derivatives as novel antitumor agents[J]. Chinese Chemical Letters,
;2014, 25(7): 978-982.
doi:
10.1016/j.cclet.2014.03.043
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A series of novel E-ring modified evodiamine derivatives were designed and synthesized as antitumor agents. Their capacity to interfere with the catalytic activity of topoisomerase I and II was evaluated by the relaxation assay. In vitro antitumor activity results revealed that compound 12 showed good antitumor activity with a broad spectrum. Its binding modes with topoisomerase I and II were clarified by molecular docking.
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