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本文报道以苯肼为原料合成了6个2-苯基-3-草酰胺基吲哚衍生物1a~f,其结构均未见文献报道。经初步体外试验结果表明,所被测试的6个目标化合物均具一定的离体黄体细胞生长抑制活性,且2-(4-甲氧苯基)吲哚化合物1b~d的活性明显高于2-苯基吲哚化合物1a。但在1b的吲哚氮上引入甲基或异丙基对活性没有影响。
In this paper, six 2-phenyl-3-oxamidoindole derivatives 1a ~ f were synthesized from phenylhydrazine as raw materials, and their structures were not reported in the literature. The results of preliminary in vitro experiments showed that all the six target compounds tested had certain cytotoxicity in vitro and the activities of 2- (4-methoxyphenyl) indole compounds 1b-d were significantly higher than those of 2 -phenylindole compound 1a. However, the introduction of methyl or isopropyl on the indole nitrogen of 1b has no effect on the activity.