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 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.