Synthesis and biological activity of esters in the trans-1,2-dihydroxy-1,2-dihydroacronycine series

被引:25
作者
Magiatis, P
Mitaku, S
Skaltsounis, AL [1 ]
Tillequin, F
Koch, M
Pierré, A
Atassi, G
机构
[1] Univ Athens, Lab Pharmacognosy, GR-15771 Athens, Greece
[2] Univ Paris 05, Fac Sci Pharmaceut & Biol, Lab Pharmacognosie, CNRS,URA 1310, F-75006 Paris, France
[3] Inst Rech Servier, F-92150 Suresnes, France
来源
JOURNAL OF NATURAL PRODUCTS | 1998年 / 61卷 / 02期
关键词
D O I
10.1021/np970427s
中图分类号
Q94 [植物学];
学科分类号
071001 ;
摘要
Permanganate oxidation of acronycine (1) led to keto alcohol 4 which could be reduced to trans-1,2-dihydroxy-1,2-dihydroacronycine (3) using NaBH4. Acylation of 3 afforded 12, 13, and 14. These esters (12, 13, and 14) were more potent than 1 when tested against L-1210 cells in vitro. Diacetate 12 was evaluated in vivo against murine P-388 leukemia and was markedly active at a dose 16-fold lower than acronycine itself. Comparison of these results with those recently obtained in the cis-1,2-dihydroxy-1,2-dihydroacronycine series is discussed.
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收藏
页码:198 / 201
页数:4
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