Nitrones have been found to exhibit attractive biological values as immuno spin trapping agents. However, successful clinical cases of nitrone therapeutics are still lacking. Herein we report the synthesis and antiproliferative activity of a series of structurally diverse nitrone derivatives against a panel of 5 cancer cell lines, based on which indole- and pyrrole-fused were further evaluated by analogue preparation and in-vitro screening. Analogues with moderate to good potency were identified. This study shows the promise for further pursuit of nitrone-type small molecules in chemotherapy.

中文翻译：

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环状硝酮衍生物作为潜在抗癌药的合成与评价

已发现亚硝基作为免疫自旋捕获剂具有诱人的生物学价值。然而，仍然缺少成功的硝酮治疗的临床案例。本文中，我们报道了一系列结构多样的硝酮衍生物对5种癌细胞系的合成和抗增殖活性，在此基础上，通过类似物制备和体外筛选进一步评估了吲哚和吡咯融合。鉴定出具有中等至良好效力的类似物。这项研究显示了在化学疗法中进一步追求硝酮类小分子的希望。