ABT-751衍生物的合成及其抗肿瘤活性的研究
Synthesis and cytotoxicity research of ABT- 751 derivatives
作者：刘雯静;曹素芬;段文虎;
Author：
收稿日期： 年卷（期）页码：2014,29(01):-5-8
期刊名称：华西药学杂志
Journal Name：WEST CHINA JOURNAL OF PHARMACEUTICAL SCIENCES
关键字：ABT-751衍生物;合成;抗肿瘤;构效关系
Key words：
基金项目：
中文摘要
目的探索ABT-751衍生物的构效关系,寻找抗肿瘤活性高的化合物。方法以2-氯-3-硝基吡啶为原料与芳基伯胺反应,胺化产物经过硝基还原和芳基磺酰反应,得到新ABT-751的衍生物;用磺酰罗丹明(SRB)法测定新衍生物对人肺癌细胞A549的增殖抑制活性。结果与结论合成了18个ABT-751衍生物,初步体外的抗肿瘤活性显示:化合物Ⅴk、Ⅴo和Ⅴq的IC50分别为0.99、0.67、0.05μmol·L-1,具良好的体外抗肿瘤活性。
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