Signal transducer and activator of transcription (STAT3) is a proposed therapeutic target for the development of anti-cancer agents. In this report, a series of N-arylsulfonylsubstituted-1H indole derivatives were designed and synthesized as STAT3 inhibitors, their anti-proliferative activities were evaluated against a number of tumor cells, some potent compounds exhibited IC₅₀ values less than 10 μM. The most potent compound 4a was further confirmed to inhibit STAT3 phosphorylation at Tyr705. It was further revealed that 4a arrested the cell cycle at the G2/M phase and inhibited tubulin polymerization. This study describes a series of N-arylsulfonylsubstituted-1H indole derivatives as potent anti-cancer agents targeting both STAT3 and tubulin.

信号转导子和转录激活子（STAT3）是开发抗癌药物的拟议治疗靶标。在本报告中，设计并合成了一系列N-芳基磺酰基取代的1 H吲哚衍生物作为STAT3抑制剂，评估了它们对多种肿瘤细胞的抗增殖活性，一些有效化合物的IC ₅₀值小于10μM。进一步证实最有效的化合物4a在Tyr705处抑制STAT3磷酸化。进一步揭示4a使细胞周期停滞在G2 / M期并抑制微管蛋白聚合。这项研究描述了一系列的N-芳基磺酰基取代的1H 吲哚衍生物作为针对STAT3和微管蛋白的有效抗癌药。