Essential structural features of acetogenins: role of hydroxy groups adjacent to the bis-THF rings

被引:22
作者
Abe, M [1 ]
Kenmochi, A [1 ]
Ichimaru, N [1 ]
Hamada, T [1 ]
Nishioka, T [1 ]
Miyoshi, H [1 ]
机构
[1] Kyoto Univ, Grad Sch Agr, Div Appl Life Sci, Sakyo Ku, Kyoto 6068502, Japan
关键词
D O I
10.1016/j.bmcl.2003.11.021
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
The presence of two hydroxy groups adjacent to the THF ring(s) is a common structural feature of natural acetogenins. To elucidate the role of each hydroxy group in the inhibitory action of acetogenins, we synthesized three acetogenin analogues which lack either or both of the hydroxy groups, and investigated their inhibitory activities with bovine heart mitochondrial complex I. Our results indicate that the presence of either of the two hydroxy groups sufficiently sustains a potent inhibitory effect. (C) 2003 Elsevier Ltd. All rights reserved.
引用
收藏
页码:779 / 782
页数:4
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