Synthesis and cytotoxicity evaluation of fluorinated brusatol, bruceosin, and dehydrobrusatol

被引:0
作者
Hitotsuyanagi, Yukio [1 ]
Yokoyama, Ryotaro [1 ]
Ren, Huiyu [1 ]
Nojima, Daiki [1 ]
Tokumaru, Yu [1 ]
Hasuda, Tomoyo [1 ]
机构
[1] Tokyo Univ Pharm & Life Sci, Sch Pharm, 1432 1 Horinouchi, Hachioji, Tokyo 1920392, Japan
关键词
Brusatol; Quassinoid; Semi-synthesis; Fluoro analogue; Cytotoxicity;
D O I
10.1016/j.rechem.2023.100988
中图分类号
O6 [化学];
学科分类号
0703 ;
摘要
Three fluorinated quassinoid analogues-4 & alpha;-fluorobruceosin, 1 & alpha;-fluorobrusatol, and 1-fluorodehydro-brusatol-were synthesized from brusatol, bruceosin, and dehydrobrusatol, respectively, by treatment with Selectfluor. These analogues were less cytotoxic to HL-60 cells than their non-fluorinated counterparts.
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页数:4
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