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6-或7-(取代苯乙烯基)香豆素类化合物的合成及其抗癌活性的研究
引用本文:徐嵩,徐世平,李兰敏.6-或7-(取代苯乙烯基)香豆素类化合物的合成及其抗癌活性的研究[J].药学学报,2000,35(2):103-107.
作者姓名:徐嵩  徐世平  李兰敏
作者单位:中国医学科学院、中国协和医科大学药物研究所,北京,100050
摘    要:目的:设计合成一系列苯乙烯基香豆素类化合物,并通过药理筛选寻找具有抗肿瘤活性的药物。方法:通过相转移Wittig反应得到目的物,利用几种药理模型进行体外抗肿瘤活性筛选。结果:合成了30个(I1~III6)新的苯乙烯基香豆素类化合物并确定其构型。结论:药理筛选结果表明,7个化合物(I2,I4,II2,II2c,III1a,III2a,III5a)对L-1210,HL-60,HCT-8,KB和Bel-7402细胞株有效,显示了一定的抗肿瘤活性。

关 键 词:苯乙烯基香豆素  抗肿瘤作用  相转移Wittig反应  顺反异构体
收稿时间:1999-05-13
修稿时间::

SYNTHESIS OF 6- OR 7-STYRYLCOUMARIN DERIVATIVES AND THEIR ANTITUMOR ACTIVITIES
Xu Song,Xu Shiping,Li Lanmin.SYNTHESIS OF 6- OR 7-STYRYLCOUMARIN DERIVATIVES AND THEIR ANTITUMOR ACTIVITIES[J].Acta Pharmaceutica Sinica,2000,35(2):103-107.
Authors:Xu Song  Xu Shiping  Li Lanmin
Abstract:AIM: A series of styrylcoumarin derivatives had been designed in order to find compounds of antitumor activities by screening in vitro. METHODS: Title compounds (I1~III6) were synthesized by phase-transfer Wittig reaction and screened by several antitumor models in vitro. RESULTS: Thirty new compounds of 6- or 7-styrylcoumarin(I1~III6) were synthesized and their configurations were determined. Seven compounds(I2,I4,II2,II2c,III1a,III2a and III5a) showed different inhibitory effects on L-1210, HL-60, HCT-8, KB and Bel-7402 cell lines in vitro. CONCLUSION: Some 6- or 7-styrylcoumarin derivatives showed antitumor activities and is worth further study.
Keywords:styrylcoumarin  antitumor  phase  transfer  Wittig  reaction  Cis  and  Trans    isomer  
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