目的 設(shè)計并合成了二茂鐵基查耳酮類化合物,并對其抗乳腺癌活性進(jìn)行研究。方法 通過Claisen-Schmidt縮合反應(yīng)合成含有二茂鐵基的查耳酮類化合物,并通過MTT法對目標(biāo)化合物的抗乳腺癌活性進(jìn)行研究。結(jié)果 合成了9個含有二茂鐵基查耳酮類化合物,其結(jié)構(gòu)均通過¹H-NMR、¹³C-NMR進(jìn)行了表征。生物活性結(jié)果表明,目標(biāo)化合物1～9對MCF-7和MDA-MB-23均具有較強(qiáng)的抑制活性,其中化合物6對MDA-MB-231的抑制活性最強(qiáng)。結(jié)論 本研究為開發(fā)具有抗荷爾蒙非依賴型乳腺癌活性的查耳酮類化合物提供了參考。

Objective To design and synthesize ferrocenyl chalcone compounds, and to study their anti-breast cancer activities. Methods A series of ferrocenyl chalcones were synthesized by Claisen-Schmidt condensation reaction, and the anti-breast cancer activity was assessed by MTT method. Results Nine ferrocenyl chalcone compounds were synthesized and characterized by ¹H-NMR and ¹³C-NMR. The preliminary biological results showed that target compounds 1 — 9 displayed significant inhibitory activities on both MCF-7 and MDA-MB-231 cell lines. Specifically, compound 6 showed the best inhibitory activity against MDA-MB-231. Conclusion This study provides reference for development of chalcone compounds with inhibitory activity in hormone-independent breast cancer.