Asperphenamate衍生物的合成及体外抗乳腺癌活性评价

目的 设计合成天然产物asperphenamate衍生物。并对其体外抗人乳腺癌作用进行评价。方法 以L-苯丙氨酸为起始原料，经过4 步反应得到目标产物，其结构经核磁共振氢谱确证。采用MTT方法，以T47D和MDA-MB231细胞为实验瘤株进行体外抗乳腺癌活性测试。结果与结论 设计合成了27个新化合物。体外抗乳腺癌活性测试结果表明，化合物NPED-6和NPED-19的体外抗乳腺癌活性明显强于苯丙氨酸片段手性中心消旋的asperphenamate，它们的半数抑制浓度接近10 μmol·L^-1。

Synthesis of asperphenamate derivatives and their anti-breast cancer activity evaluation

Aim To design and synthesize some asperphenamate derivatives which the phenylalanine moiety racemized and to evaluate their anti-breast cancer activity in vitro.Methods Starting from L-phenylalanine,the target compounds were prepared through four steps.Their structures were confirmed by 1H-NMR.Their anti-breast cancer activities were evaluated by MTT method using the T47D and MDA-MB231 cell lines.Results and conclusion Twenty-seven compounds not reported were synthesized successfully.NPED-6 and NPED-19 show...