【摘 要】
：
抑制尿激酶型纤溶酶原激活物(u-PA)可以阻止一系列病理过程,如：肿瘤细胞粘附、迁移和在转移部位的生长.本文设计合成并评价了新的u-PA抑制剂：SS,RR,RS和SR 3-(4-氨基丁基)-6-(1H-吲哚-3-甲基)哌嗪-2,5-二酮(AIPZ).手性高效液相色谱显示,它们的纯度接近100％.将这些类似物和u-PA活性位点进行对接,均得到较高的分数(118-134).FT-MS表明,在水溶液中A
【机 构】
：
首都医科大学化学生物学与药学院,北京市,100069
【出 处】
：
首都医科大学第四届研究生学术论坛第二分论坛
论文部分内容阅读
抑制尿激酶型纤溶酶原激活物(u-PA)可以阻止一系列病理过程,如：肿瘤细胞粘附、迁移和在转移部位的生长.本文设计合成并评价了新的u-PA抑制剂：SS,RR,RS和SR 3-(4-氨基丁基)-6-(1H-吲哚-3-甲基)哌嗪-2,5-二酮(AIPZ).手性高效液相色谱显示,它们的纯度接近100％.将这些类似物和u-PA活性位点进行对接,均得到较高的分数(118-134).FT-MS表明,在水溶液中AIPZ的SS,RR,RS与SR构型分别以二聚体,四聚体,三聚体,三聚体存在.利用二维核磁共振图谱ROESY确定了二聚体,三聚体,四聚体的不同构象.透射电子显微镜(TEM)和扫描电子显微镜(SEM)观察结果表明,SS,RR,RS和SR可以形成不同的纳米结构.
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