Asperphenamate衍生物的合成及体外抗乳腺癌活性评价  

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

作　　者：袁雷[1] 李云飞[1] 孙铁民[1] 

机构地区：[1]沈阳药科大学制药工程学院,辽宁沈阳110016

出　　处：《中国药物化学杂志》2010年第5期336-341,共6页Chinese Journal of Medicinal Chemistry

基　　金：国家自然科学基金项目(30472190)

摘　　要：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 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 showed stronger activity against two kinds of cell lines than asperphenamate whose phenylalanine moiety racemized.Their IC50 values approach 10 μmol·L-1.

关 键 词：消旋化 asperphenamate 抗乳腺癌活性 MTT法 

分 类 号：R914[医药卫生—药物化学]