贾美琪;刘菁菁;聂江平;段宏泉;秦楠;

• 1:天津医科大学药学院
• 2:天津医科大学基础医学研究中心

摘要(Abstract)：

目的设计并合成紫罗兰酮生物碱异唑类衍生物,结合活性筛选,发现具有活性的新型紫罗兰酮生物碱衍生物。方法制备(R)-紫罗兰酮,在此基础上经过11步有机合成反应制备紫罗兰酮生物碱异唑衍生物。目标衍生物经核磁共振波谱和高分辨质谱表征其化学结构。通过乳腺癌细胞趋化迁移实验筛选衍生物的抗肿瘤转移活性。结果共制备8个目标衍生物,经抗肿瘤转移活性筛选发现,化合物12c活性同Ion-31a相当,强于阳性对照化合物PI3K抑制剂LY294002。结论所有目标衍生物均为新化合物,其中苯甲腈取代异唑化合物12c具有显著抗肿瘤转移活性。

关键词(KeyWords)： 手性紫罗兰酮生物碱;异唑;乳腺癌;抗肿瘤转移

Abstract:

Keywords:

基金项目(Foundation): 国家自然科学基金面上项目（81673310）;; 天津市自然科学基金资助项目（17JCZDJC32900）

作者(Author): 贾美琪;刘菁菁;聂江平;段宏泉;秦楠;

Email:

DOI:

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