Chemical modification of alisol B23-acetate and their cytotoxic activity

被引：12
作者：
Lee, S
Min, B
Bae, K [1 ]
机构：
[1] Chungnam Natl Univ, Coll Pharm, Taejon 305764, South Korea
[2] Korea Res Inst Biosci & Biotechnol, Taejon 305600, South Korea
来源：
ARCHIVES OF PHARMACAL RESEARCH | 2002年 / 25卷 / 05期
关键词：
Alismatis Rhizoma; protostane; cytotoxic activity;
D O I：
10.1007/BF02976929
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
The twelve-protostane analogues were synthesized from alisol B 23-acetate and assessed for their in vitro antitumor activity against six different human and murine tumor cell lines. Of the compounds synthesized, 23S-acetoxy-24R(25)-epoxy-11beta,23S-dihydroxyprotost-13(17)-en-3-hy-droxy-imine (12) exhibited significant cytotoxic activities;against A549, SK-OV3, B16-F10, and HT1080 tumor cells with ED50 values of 10.0, 8.7, 5.2, and 3.1 mug/ml, respectively. Furthermore, 23S-acetoxy-13(17),24R(25)-diepoxy-11beta-hydroxyprotost-3-one(5), 13(17),24R(25)-diepoxy-11beta,23S-dihydroxyprotostan-3-one (6), 24R,25-epoxy-11beta,23S-dihydroxyprotost-13(17)-en-3-one (7), and 11beta, 23S,24R,25-tetrahydroxyprotost-13(17)-en-3-one (9) showed moderate cytotoxic activities against B16-F10 and HT1080 tumor cells. These results mean that a hydroxyimino group at C-3 position in the protostane-type terpene enhances cytotoxic activity.
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收藏
页码：608 / 612
页数：5
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