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| Synthesis and cytotoxic activity of novel 2, 6-disubstituted-4-mor- pholinothieno[3, 2-d]pyrimidines as potent anti-tumor agents |
| Wu Fu Zhu, Xin Zhai, Sai Li, Yun Yun Cao, Ping Gong, Ya Jing Liu * |
| Key Laboratary of Original New Drugs Design and Discovery of Ministry of Education, School of Pharmaceutical Engineering, Shenyang Pharmaceutical University, Shenyang 110016, China |
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Abstract 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 μmol/L, 0.23 μmol/L, 2.52 μmol/L, 1.80 μmol/L) was 1.1, 2.9, 29,3 and 4.3 times more active than GDC-0941 (0.87 μmol/L, 0.66 μmol/L, 73.8 μmol/L, 7.77 μmol/L) against H460, HT-29, MDA-MB-231 and U87MG cell lines, respectively.
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