Organofluorines are a group of fluorinated substances with broad application as pharmaceuticals, agrochemicals and polymers. We designed and synthesized a series of new biologically active trifluoromethyl containing indole derivatives. Target 2´-aminoanalogs and 2,2´-diaminoanalogs of 1-methoxyspirobrassinol methyl ether bearing (4-trifluoromethylphenylamino) or 3,5-bis(trifluoromethyl)phenylamino moiety were prepared by spirocyclization methodology. The newly synthesized indole analogs display higher potency of antiproliferative effect against eight human leukemia and solid tumor cell lines than their parental natural phytoalexin. The most potent antiproliferative agents were 2,2´-diaminoanalogs possessing two 3,5-bis(trifluoromethyl)phenylamino groups, which displayed higher potency than cisplatin against screened cancer cell lines, but at the same time lower cytotoxicity than cisplatin on non-malignant murine fibroblasts NIH 3T3.

有机氟是一组氟化物，广泛用作药物，农用化学品和聚合物。我们设计和合成了一系列新的具有生物活性的含三氟甲基吲哚衍生物。通过螺环化方法制备了带有1-甲氧基螺spir菜油醇甲基醚（4-三氟甲基苯基氨基）或3,5-双（三氟甲基）苯基氨基部分的目标2′-氨基类似物和2，2′-二氨基类似物。新合成的吲哚类似物比其亲本天然植物抗毒素显示出对八种人类白血病和实体瘤细胞系更高的抗增殖作用。最有效的抗增殖剂是具有两个3,5-双（三氟甲基）苯基氨基的2,2′-二氨基类似物，对筛选的癌细胞系显示出比顺铂更高的效能，