二芳醚基哌嗪类衍生物的合成及细胞毒活性研究

Synthesis of Diaryl Ether Substituted Piperazine Derivatives and Their Cytotoxic Activities

根据拼合原理,设计并合成了21个未见报道的新的二芳醚基哌嗪类衍生物,其结构用1H NMR,ESI-MS,HRMS进行了确证,初步生物活性测定实验证明部分目标化合物具有良好的细胞毒活性.化合物4i分别对人食管癌(Eca109)细胞株和人鼻咽癌(CNE)细胞株的IC50为7.13和4.54μmol·L-1,与对照品顺铂(DDP)相近.化合物5d对人鼻咽癌细胞株也表现较好的活性,其IC50为8.49μmol·L-1.

Twenty-one new diaryl ether substituted piperazine derivatives were synthesized and their structures were confirmed by 1H NMR, ESI-MS and HRMS data. The preliminary biological activity tests showed that some of the tire compounds had good activities. Compound 4i exhibited a potent cytotoxicity against the Eca109 and CNE cell lines with IC50 values of 7.13 and 4.54 μmol·L^-1, respectively, which showed the similar activities to the positive control, cisplatin. Compound 5d also possessed an efficient cytotoxicity aganist CNE cell lines with an IC50 value of 8.49 μmol·L^-1.