2-Desoxy-4-epi-puchellin (PCL) is a sesquiterpene-lactone, which naturally occurs in many traditional Chinese medicinal plants, and has antitumor and anti-inflammatory activities. In this work, a series of 13-amino derivatives of PCL were synthesized through Michael addition reaction. Inhibition of IL-6-induced STAT3 signaling pathway and in vitro cytotoxicity of these compounds were evaluated, and their effect on the cell cycle was also studied. The methyl hydroxyethylamine derivatives showed higher potency than PCL, which could induce significant mitotic arrest via G2/M arrest in HCT116 cancer cells, indicating that these derivatives have the potential to be developed into anti-colon cancer drugs.

中文翻译：

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天然产物13-氨基2-脱氧4-表普尿素的合成衍生物抑制STAT3信号传导，并诱导结肠癌细胞G2 / M阻滞和死亡。

2-Desoxy-4-epi-puchellin（PCL）是倍半萜内酯，天然存在于许多传统中草药中，具有抗肿瘤和抗炎作用。在这项工作中，通过迈克尔加成反应合成了一系列PCL的13-氨基衍生物。评估了这些化合物对IL-6诱导的STAT3信号通路的抑制作用和体外细胞毒性，并研究了它们对细胞周期的影响。甲基羟乙基胺衍生物显示出比PCL高的效力，后者可通过G2 / M阻滞在HCT116癌细胞中诱导明显的有丝分裂阻滞，表明这些衍生物具有被开发为抗结肠癌药物的潜力。