4-,6-或7-位取代苯基亚胺次甲基香豆素的合成及其抗癌活性

SYNTHESIS OF 4-, 6- OR 7- SUBSTITUTED PHENYLIMINOMETHYLENECOUMARINS AND THEIR ANTICANCER ACTIVITIES

摘要: 目的设计合成一系列香豆素西佛碱化合物并进行抗癌筛选。方法合成了21个取代的4-,6-或7-位苯基亚胺次甲基香豆素,其结构经MS,HNMR和元素分析确证,并对其进行体外抗癌筛选。结果12个化合物(3c,3d,3e,3f,3g,3h,3j,3k,3m,3o,3p,3q)分别对KB,HCT-8,Bel7402细胞株有效。结论该类化合物有一定抗癌活性,值得进一步研究。

Abstract: AIMA series of substituted phenyliminomethylenecoumarins derivatives was designed in order to find compounds possessing anticancer activities. METHODSTitle compounds (1a～b, 2a～b and 3a～q) were synthesized and screened by several anticancer models in vitro. RESULTSTwenty-one new compounds (1a～b, 2a～b and 3a～q) were synthesized and screened. Structrues of the new compunds were determined by MS, HNMR and elemental analysis. Twelve compounds (3c, 3d, 3e, 3f, 3g, 3h, 3j, 3k, 3m, 3o, 3p, 3q) showed inhibitory effects on HCT-8, KB and Bel7402 cell lines in vitro. CONCLUSIONSome compounds had certain anticancer activities and were worth further studying.