In order to improve the antitumor potency of the natural product evodiamine, novel boron-containing evodiamine derivatives were designed by incorporating boronic acid and boronate as trigger units. Boronate derivative 13a could be triggered by reactive oxygen species (ROS) in the HCT116 colon cancer cell line and showed excellent antitumor activity in vitro and in vivo. It induced apoptosis in HCT116 cancer cells in a dose-dependent manner and cell growth arrest at the G2 phase.

中文翻译：

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具有硼酸盐触发单元的天然产物Evodiamine：发现有效的抗结肠癌抗肿瘤药。

为了提高天然产物evodiamine的抗肿瘤效力，通过掺入硼酸和硼酸酯作为触发单元来设计新型的含硼的evodiamine衍生物。硼酸盐衍生物13a可以由HCT116结肠癌细胞系中的活性氧（ROS）触发，并在体内和体外显示出优异的抗肿瘤活性。它以剂量依赖性方式诱导HCT116癌细胞凋亡，并使细胞生长停滞在G2期。