Synthesis and cytotoxic activity of novel 2,6-disubstituted-4-mor-pholinothieno[3,2-d]pyrimidines as potent anti-tumor agents

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• 作者：Wu Fu Zhu ; Xin Zhai ; Sai Li ; Yun Yun Cao ; Ping Gong ; Ya Jing Liu ; ^{lyjpharm@126.com}
• 关键词：4-Morpholinothieno[3 ; 2-d]pyrimidine ; Synthesis ; Cytotoxic activity
• 刊名：Chinese Chemical Letters
• 出版年：2012
• 期刊代码：3_10018417
• 类别：ch
• 出版时间：June, 2012
• 卷：23
• 期：6
• 页码：703-706
• 文件大小：732 K

摘要

A series of 2,6-disubstituted-4-morpholinothieno[3,2-d]pyrimidine derivatives were synthesized and their cytotoxic activity against H460, HT-29, MDA-MB-231, U87MG and H1975 cancer cell lines were evaluated in vitro. Most of the target compounds exhibited moderate to excellent activity to the tested cell lines. The most promising compound lass="boldFont">23 (0.84 渭mol/L, 0.23 渭mol/L, 2.52 渭mol/L, 1.80 渭mol/L) was 1.0, 2.9, 29.3 and 4.3 times more active than GDC-0941 (0.87 渭mol/L, 0.66 渭mol/L, 73.8 渭mol/L, 7.77 渭mol/L) against H460, HT-29, MDA-MB-231 and U87MG cell lines, respectively.