新型螺环氧化吲哚-吡咯烷化合物：合成、抗癌及分子对接研究
Novel spirooxindole-pyrrolidine compounds: synthesis, anticancer and molecular docking studies.
作者信息
Arun Y, Saranraj K, Balachandran C, Perumal P T
机构信息
Organic Chemistry Division, CSIR-Central Leather Research Institute, Chennai 600020, India.
Division of Microbiology and Cancer Biology, Entomology Research Institute, Loyola College, Chennai 600034, India.
出版信息
Eur J Med Chem. 2014 Mar 3;74:50-64. doi: 10.1016/j.ejmech.2013.12.027. Epub 2014 Jan 3.
Novel spirooxindole-pyrrolidine compounds have been synthesised through 1,3-dipolar cycloaddition of azomethine ylides generated from isatin and sarcosine or thioproline with the dipolarophile 3-(1H-imidazol-2-yl)-2-(1H-indole-3-carbonyl)acrylonitrile under the optimised reaction condition. Synthesised compounds were evaluated for their anticancer activity against A549 human lung adenocarcinoma cancer cell line. Among the 29 tested compounds 4j, 6b and 6h showed very high activity 66.3%, 64.8% and 66.3% at 25 μg/mL concentration against A549 lung adenocarcinoma cancer cell line. These spirooxindole-pyrrolidine compounds can be promising therapeutic agents for A549 lung adenocarcinoma cancer cell line.
在优化的反应条件下，通过异吲哚酮与肌氨酸或硫代脯氨酸生成的甲亚胺叶立德与亲偶极体3-(1H-咪唑-2-基)-2-(1H-吲哚-3-羰基)丙烯腈进行1,3-偶极环加成反应，合成了新型螺环氧化吲哚-吡咯烷化合物。对合成的化合物针对A549人肺腺癌细胞系的抗癌活性进行了评估。在29种受试化合物中，4j、6b和6h在25μg/mL浓度下对A549肺腺癌细胞系表现出非常高的活性，分别为66.3%、64.8%和66.3%。这些螺环氧化吲哚-吡咯烷化合物有望成为治疗A549肺腺癌细胞系的药物。
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