取代4-苯乙烯基香豆素的合成及其抗肿瘤活性

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-60,KB,HCT-8和Bel-7402进行体外细胞毒活性筛选。结果所合成的20个(1-20)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。

SYNTHESIS OF SUBSTITUTED 4-STYRYLCOUMARIN AND THEIR ANTITUMOR ACTIVITIES

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.