目的 設(shè)計(jì)并合成圓柚酮生物堿衍生物，篩選具有抗乳腺癌遷移活性的化合物。方法 以圓柚酮為起始原料，通過氯化反應(yīng)、氧化反應(yīng)、親核取代和還原胺化得到目標(biāo)化合物。通過MDA-MB-231細(xì)胞的抗遷移實(shí)驗(yàn)檢測(cè)化合物抗腫瘤轉(zhuǎn)移活性。結(jié)果 共合成11個(gè)圓柚酮生物堿衍生物，化合物2e、4b、4d抗乳腺癌轉(zhuǎn)移活性較強(qiáng)。結(jié)論 合成了具有抗腫瘤轉(zhuǎn)移作用的圓柚酮生物堿衍生物，為乳腺癌轉(zhuǎn)移藥物的開發(fā)提供了依據(jù)。

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

國家自然科學(xué)基金面上項(xiàng)目（81673310）