吲哚 C5-N 取代基对 secoduocarmycin 类似物细胞毒性的结构影响。
Structural influence of indole C5-N-substitutents on the cytotoxicity of seco-duocarmycin analogs.
机构信息
College of Pharmacy, Catholic University of Daegu, Hayang, Korea.
出版信息
Arch Pharm Res. 2011 Mar;34(3):357-67. doi: 10.1007/s12272-011-0302-1. Epub 2011 May 6.
A series of racemic indole C5-substituted seco-cyclopropylindoline compounds (2,3 and 5-7) were prepared by coupling 1-(tert-butyloxycarbonyl)-3-(chlorocarbonyl)indoline (seg-A) with 5,6,7-trimethoxy-, 5,6-dimethoxy-, 5-amino-, 5-methylsulfonylamino- and 5-(N,N-dimethylaminosulfonylamino) indole-2-carboxylic acid as seg-B in the presence of 1-ethyl-3-(3-dimethylaminopropyl) carbodiimide. The synthetic compounds (2,3 and 5-7) were tested for cytotoxic activity against human cancer cell lines (COLO 205, SK-MEL-2, A549, and JEG-3) using the MTT assay.
一系列外消旋吲哚 C5-取代的 sec-环丙基吲哚啉化合物（2、3 和 5-7）是通过将 1-（叔丁氧羰基）-3-（氯羰基）吲哚啉（seg-A）与 5,6,7-三甲氧基-、5,6-二甲氧基-、5-氨基-、5-甲磺酰氨基-和 5-（N,N-二甲基氨基磺酰基氨基）吲哚-2-羧酸在 1-乙基-3-（3-二甲基氨基丙基）碳二亚胺的存在下偶联制备的。使用 MTT 测定法，测试了合成化合物（2、3 和 5-7）对人癌细胞系（COLO 205、SK-MEL-2、A549 和 JEG-3）的细胞毒性活性。
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