Asperphenamate全合成新方法及体外抗乳腺癌活性评价  

New total synthesis of asperphenamate and its anti-breast cancer activity evaluation in vitro

作　　者：袁雷[1] 谢集照[1] 张聪[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》2008年第3期186-189,共4页Chinese Journal of Medicinal Chemistry

基　　金：国家自然科学基金项目(30472190)

摘　　要：目的探索活性天然产物asperphenamate全合成的新方法,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7步反应得到光学活性的目标产物,其结构经红外光谱、CD光谱、核磁共振氢谱、ESI-MS及旋光度确证。采用MTT法,对雌激素受体肿瘤细胞T47D和MDA-MB231进行体外抗乳腺癌活性测试。结果与结论以总收率34%合成了asperphenamate。体外抗乳腺癌活性测试表明asperphena-mate对两种肿瘤细胞株没有抑制活性。Aim To explore a new synthetic method of asperphenamate and evaluate its anti-breast cancer activity in vitro. Methods Starting from L-phenylalanine, target compound was prepared via a seven-steps sequence. Its structure was confirmed by IR, CD, 1^H-NMR, ESI-MS and optical rotation. Its anti-breast cancer activity was evaluated by MTT method and using the estrogen receptor cell lines T47D and MDA- MB231. Results and conclusion Compound 1 was successfully synthesized in an overall yield of 34 %. It did not show any activity against T47D and MDAMB231 cell lines.

关 键 词：asperphenamate auranamide 抗乳腺癌活牲 不对称合成 MTT法 

分 类 号：R737.9[医药卫生—肿瘤]