Previously unknown conjugates of the natural sesquiterpene lactone arteannuin B, which was isolated from Artemisia annua , were synthesized via Michael reactions with pharmacophoric amines and tested in vitro for cytotoxic activity. The compounds were shown to exhibit antiproliferative properties for various tumor cell lines. The most active derivatives had IC 50 values of 8–36 μM, which exceeded that of starting arteannuin B. Practically all obtained conjugates were found to modulate glycolysis in MCF7 tumor cells. The lead compound was the conjugate with 3-ethoxycarbonylpiperidine, which could be considered a platform for developing antitumor drugs.

中文翻译：

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新青蒿素 B 衍生物及其细胞毒活性

从青蒿中分离出的天然倍半萜内酯青蒿素 B 的先前未知的缀合物是通过与药效胺的迈克尔反应合成的，并在体外测试了细胞毒活性。这些化合物显示出对各种肿瘤细胞系的抗增殖特性。最具活性的衍生物的 IC 50 值为 8–36 μM，超过了起始青蒿素 B 的 IC 50 值。实际上发现所有获得的缀合物都可以调节 MCF7 肿瘤细胞中的糖酵解。先导化合物是与 3-乙氧基羰基哌啶的结合物，可被视为开发抗肿瘤药物的平台。