中文摘要：

从色醇出发,通过Sharpless环氧化、酰胺化、偶联和成盐四步反应合成了一系列新型的吲哚并四氢呋喃-咪唑盐杂合物,其结构经~1H NMR,~（13）CNMR,HRMS以及X射线单晶衍射确定.对合成的新化合物进行了体外抗肿瘤细胞毒活性筛选,结果表明,1-（（3aR,8aS）-3,3a-二氢-3a-羟基-2H-呋喃并[2,3-b]吲哚-8（8aH）-基）乙酮-3-（2-（萘-2-基）-2-氧乙基）-5,6-二甲基-1H-苯并[d]咪唑-3-溴盐（20）和1-（（3aR,8aS）-3,3a-二氢-3a-羟基-2H-呋喃并[2,3-b]吲哚-8（8aH）-基）乙酮-3-（2-萘甲基））-5,6-二甲基-1H-苯并[d]咪唑-3-溴盐（22）具有较好的体外肿瘤生长抑制活性,对SMMC-7721、MCF-7和SW-480肿瘤细胞株的活性均优于顺铂（DDP）,1-（（3aR,8aS）-3,3a-二氢-3a-羟基-2H-呋喃并[2,3-b]吲哚-8（8a H）-基）乙酮-3-（2-溴苄基））-5,6-二甲基-1H-苯并[d]咪唑-3-溴盐（24）对SW-480肿瘤细胞株表现出较好的选择性细胞毒活性,其IC_（50）值约为顺铂的2.0倍.

英文摘要：

A series of novel hybrid compounds between indolo[b]tetrahydrofuran and imidazolium salts were prepared from tryptophol by four steps of Sharpless epoxidation, amidation, coupling and salt formation. Their structures were confirmed by ~1HNMR, ~（13）CNMR, HRMS and X-ray crystallographic analysis. These compounds were evaluated in vitro against a panel of human tumor cell lines. The results showed that 1-（（3aR,8aS）-3,3a-dihydro-3a-hydroxy-2H-furo[2,3-b]indol-8（8aH）-yl）ethanone-3-（2-（naphthalen-2-yl）-2-oxoethyl）-5,6-dimethyl-1H-benzo[d]-imidazol-3-ium bromide（20） and 1-（（3aR,8aS）-3,3a-dihydro-3a-hydroxy-2H-furo[2,3-b]indol-8（8aH）-yl）ethanone-3-（2-naphthylmethyl）-5,6-dimethyl-1H-benzo[d]imidazol-3-ium bromide（22） exhibited higher inhibitory activity selectively against SMMC-7721, MCF-7 and SW480 cell lines compared with DDP. In particular, 1-（（3aR,8aS）-3,3a-dihydro-3a-hydroxy-2H-furo[2,3-b]indol-8（8a H）-yl）ethanone-3-（2-bromobenzyl）-5,6-dimethyl-1H-benzo[d]imidazol-3-ium bromide（24） was more selective to SW-480 cell lines with IC_（50） values 2.0-fold lower than DDP.