多样性导向合成螺环吲哚类天然产物及其初步活性的评价
Diversity-oriented syntheses of natural-like dispirooxindole derivatives and their preliminary activity evaluation
作者：徐进松;鲍锦库;
Author：
收稿日期： 年卷（期）页码：2015,30(05):-530-536
期刊名称：华西药学杂志
Journal Name：WEST CHINA JOURNAL OF PHARMACEUTICAL SCIENCES
关键字：1,3-偶极环合;亚胺叶立德;多组分反应;螺环吲哚衍生物;多样性导向合成;类天然产物;计算机辅助药物设计
Key words：
基金项目：
中文摘要
目的探索多样性导向合成类天然产物的方法,寻找具潜在药理活性的分子。方法利用各种靛红衍生物与氨基酸衍生物原位生成亚胺叶立德,在温和条件下与取代苄基-2-苯基噁唑酮发生具有区域选择性和立体选择性的1,3-偶极环化反应,一锅法生成连接噁唑酮、螺环吲哚-四氢吡咯、吡咯里西啶和吡咯并噻唑的结构复杂的类天然产物;利用计算机辅助药物设计方法鉴定潜在的靶点和已合成化合物的ADMET性质,并进行细胞活性筛选。结果建立了一种快速有效构建复杂类天然产物库的方法,经过基于计算机辅助药物设计和体外筛选的方法得到一个具有潜在抗肿瘤活性的先导化合物。结论所用方法对寻找和发现具有药理活性的先导化合物具较好的可行性。
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