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

SYNTHESIS OF 6- OR 7-STYRYLCOUMARIN DERIVATIVES AND THEIR ANTITUMOR ACTIVITIES

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～II_I6）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，I_4，II_2，II_2c，III_1a，III_2a，III_5a)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。

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(I_2，I₄，II₂，II_2c，III_1a，III_2a and III_5a) 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.