4-吗啉喹唑啉类PI3K抑制剂的合成及活性研究
Synthesis and anticancer activity of 4-morpholinoquinazolines as PI3K inhibitors
作者：高国锐;段文虎;
Author：
收稿日期： 年卷（期）页码：2013,28(03):-219-223
期刊名称：华西药学杂志
Journal Name：WEST CHINA JOURNAL OF PHARMACEUTICAL SCIENCES
关键字：PI3K抑制剂;4-吗啉喹唑啉;合成;抗肿瘤活性
Key words：
基金项目：
中文摘要
目的寻找具有新型骨架结构的磷脂酰肌醇3激酶(PI3K)抑制剂。方法基于活性化合物,利用"杂交"设计原理,设计和合成了系列4-吗啉喹唑啉类衍生物。结果目标化合物经1HNMR、质谱确证结构,并评价了其对Rh30细胞的增殖抑制活性。结论大部分化合物具有较好的抑制活性,化合物8b的活性最强,其IC50达0.8μmol.L-1。4-吗啉喹唑啉是一类新型的PI3K抑制剂骨架,值得进一步进行结构修饰研究。
英文摘要
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