کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
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1257305 | 971556 | 2015 | 5 صفحه PDF | دانلود رایگان |
Evodiamine and its derivatives have an asymmetric center at the C13b position. Herein, isomers of evodiamine derivatives 2 and 3 were obtained by straightforward asymmetric total synthesis. Their inhibitory activities toward topoisomerases I and II and their cytotoxicities in cancer cell lines were evaluated. All the four isomers exhibited good to excellent antitumor potency and the (S)-isomers were generally more active than the (R)-isomers. The binding modes of (S)-2 with topoisomerases I and II were also clarified by molecular docking.
Isomers of evodiamine derivatives 2 and 3 were obtained by straightforward asymmetric total synthesis and their antitumor activity was investigated. All the four isomers exhibited good to excellent antitumor potency.Figure optionsDownload as PowerPoint slide
Journal: Chinese Chemical Letters - Volume 26, Issue 3, March 2015, Pages 267–271