Abstract

An efficient metal free high yield method of synthesis of bis(indolyl)methanes (BIMs) and bis(aryl)alkanes analogs in the presence of B(C₆F₅)₃ by condensation of primary amines with pyruvates has been successfully developed. Some analogs of BIMs display good in vitro antitumor activity, screened by MTT assay. Compound 3b demonstrates the best anti-cancer activity against lung carcinoma cell A549 cells with IC₅₀ of 4.52 µM.

中文翻译：

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双（芳基）烷烃和双（吲哚基）甲烷生物碱类似物的简便合成和抗癌活性

摘要

已经成功地开发了一种在伯（C ₆ F ₅）₃存在下通过伯胺与丙酮酸缩合反应合成双（吲哚基）甲烷（BIM）和双（芳基）烷烃类似物的高效无金属高产率方法。通过MTT分析筛选，一些BIM类似物显示出良好的体外抗肿瘤活性。化合物3b表现出对肺癌细胞A549细胞的最佳抗癌活性，IC ₅₀为4.52 µM。