Semisynthesis of salviandulin E analogues and their antitrypanosomal activity
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- 作者：Yutaka Aoyagi ; Koji Fujiwara ; Akira Yamazaki ; Naoko Sugawara ; Reiko Yano ; Haruhiko Fukaya ; Yukio Hitotsuyanagi ; Koichi Takeya ; Aki Ishiyama ; Masato Iwatsuki ; Kazuhiko Otoguro ; Haruki Yamada ; Satoshi 艑mura
- 关键词：Semisynthesis ; Antitrypanosomal activity ; Neoclerodane diterpene ; Salvia leucantha ; Salviandulin E
- 刊名：Bioorganic and Medicinal Chemistry Letters
- 出版年：15 January, 2014
- 年：2014
- 卷：24
- 期：2
- 页码：442-446
- 全文大小：1041 K
文摘
A series of analogues of salviandulin E, a rearranged neoclerodane diterpene originally isolated from Salvia leucantha (Lamiaceae), were prepared and their in vitro activity against Trypanosoma brucei brucei was evaluated with currently used therapeutic drugs as positive controls. One of the 19 compounds prepared and assayed in the present study, butanoyl 3,4-dihydrosalviandulin E analogue was found to be a possible candidate for an antitrypanosomal drug with fairly strong antitrypanosomal activity and lower cytotoxicity.