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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10μmol.L-1。
Aim To design and synthesize asperphenamate derivatives. And its anti-human breast cancer in vitro evaluation. Methods L-phenylalanine was used as the starting material and the target product was obtained after 4 steps. The structure was confirmed by 1H NMR. MTT assay was used to test the anti-breast cancer activity of T47D and MDA-MB231 cells in vitro. RESULTS AND CONCLUSIONS 27 new compounds were designed and synthesized. In vitro anti-breast cancer activity test results show that compounds NPED-6 and NPED-19 in vitro anti-breast cancer activity was significantly stronger than phenylalanine chiral center racemic asperphenamate, their half-value concentration close to 10μmol.L-1 .