取代4-苯乙烯基香豆素的合成及其抗肿瘤活性

SYNTHESIS OF SUBSTITUTED 4-STYRYLCOUMARIN AND THEIR ANTITUMOR ACTIVITIES

目的 为寻找有抗肿瘤活性的物质 ,设计并合成了一系列取代 4 苯乙烯基香豆素化合物。方法 用相转移Wittig反应和Horner反应得目的物 ,用1HNMR ,MS和元素分析确证其结构 ;用HL 6 0 ,KB ,HCT 8和Bel 740 2进行体外细胞毒活性筛选。结果 所合成的 2 0个 ( 1- 2 0 ) 4 苯乙烯基香豆素为新化合物。化合物 18对KB细胞株有效。结论 化合物 18显示了抗肿瘤活性 ,值得进一步研究。

AIM A series of 4-styrylcoumarin derivatives had been designed and synthesized in order to find compounds of antitumor activities by screening. METHODS Title compounds (1-20) were synthesized by Phase-Transfer Wittig reaction or Wittig-Horner reaction, and screened by several antitumor models in vitro . Their structures were determined by 1HNMR, MS and elemental analysis. RESULTS Twenty compounds (1-20) are new compounds. Compound 18 had effects on KB cell lines in vitro . CONCLUSION It was seen that compound 18 had certain antitumor activities, and it was worth further studying.