目的 设计并合成圆柚酮生物碱衍生物，筛选具有抗乳腺癌迁移活性的化合物。方法 以圆柚酮为起始原料，通过氯化反应、氧化反应、亲核取代和还原胺化得到目标化合物。通过MDA-MB-231细胞的抗迁移实验检测化合物抗肿瘤转移活性。结果 共合成11个圆柚酮生物碱衍生物，化合物2e、4b、4d抗乳腺癌转移活性较强。结论 合成了具有抗肿瘤转移作用的圆柚酮生物碱衍生物，为乳腺癌转移药物的开发提供了依据。

Objective To design and synthetize nootkatone alkaloid derivatives, and screen compounds with anti-metastatic activity against breast cancer. Methods Starting from nootkatone, the target compounds were obtained through chlorination reaction, oxidation reaction, nucleophilic substitution, and reductive amination. The anti-tumor metastasis activity of the compound through anti-migration experiments on MDA-MB-231 cells was performed. Results A total of 11 nootkatone alkaloid derivatives were synthesized, and compounds 2e, 4b, and 4d showed strong anti-migration activity against breast cancer cells. Conclusion The nootkatone alkaloid derivatives with anti-tumor metastasis activity are synthesized, which can provided a basis for the development of breast cancer metastasis drugs.

R914

国家自然科学基金面上项目（81673310）