Synthesis and antitumor activities of a new series of 4,5-dihydro-1H-thiochromeno4,3-dpyrimidine derivatives | |
Alternative Title | Synthesis and antitumor activities of a new series of 4,5-dihydro-1H-thiochromeno4,3-dpyrimidine derivatives |
Guo DeXiang; Liu YaJing; Li Ting; Wang Nan; Zhai Xin; Hu Chun; Gong Ping | |
2012 | |
Source Publication | SCIENCE CHINA-CHEMISTRY
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ISSN | 1674-7291 |
Volume | 55Issue:3Pages:347-351 |
Abstract | A new series of 4,5-dihydro-1H-thiochromeno4,3-dpyrimidine derivatives have been designed and synthesized. The antitumor activities of the target compounds have been evaluated in vitro against two human cancer cell lines including A549 (human alveolar adenocarcinoma cell) and H460 (human lung cancer) by MTT assay. Most of the target compounds exhibited significant antitumor activities against A549 and H460 cancer cell lines. The most potent compound 4-(benzod1,3dioxol-5-yl)-8,9-difluoro-2-(4-methylpiperazin-1-yl)-4,5-dihydro-1H-thiochromeno4,3-dpyrimidine (CH05) (IC50 = 0.44 mu M, 3.07 mu M) was 2.0 and 8.4 times more active than gefitinib (IC50 = 0.89 mu M, 16.81 mu M) against A549 and H460 cell lines, respectively. |
Other Abstract | A new series of 4,5-dihydro-1H-thiochromeno4,3-dpyrimidine derivatives have been designed and synthesized.The antitumor activities of the target compounds have been evaluated in vitro against two human cancer cell lines including A549 (human alveolar adenocarcinoma cell) and H460 (human lung cancer) by MTT assay.Most of the target compounds exhibited significant antitumor activities against A549 and H460 cancer cell lines.The most potent compound 4-(benzod1,3dioxol5-yl)-8,9-difluoro-2-(4-methylpiperazin-1-yl)-4,5-dihydro-1H-thiochromeno4,3-dpyrimidine (CH05) (IC50=0.44 M,3.07 M) was 2.0 and 8.4 times more active than gefitinib (IC50=0.89 M,16.81 M) against A549 and H460 cell lines,respectively. |
Keyword | heterocycle synthesis 4,5-dihydro-1H-thiochromeno4,3-dpyrimidine derivatives antitumor activity |
Indexed By | CSCD |
Language | 英语 |
Funding Project | [National Natural Science Foundation of China] |
CSCD ID | CSCD:4537942 |
Citation statistics | |
Document Type | 期刊论文 |
Identifier | http://ir.imr.ac.cn/handle/321006/147775 |
Collection | 中国科学院金属研究所 |
Affiliation | 中国科学院金属研究所 |
Recommended Citation GB/T 7714 | Guo DeXiang,Liu YaJing,Li Ting,et al. Synthesis and antitumor activities of a new series of 4,5-dihydro-1H-thiochromeno4,3-dpyrimidine derivatives[J]. SCIENCE CHINA-CHEMISTRY,2012,55(3):347-351. |
APA | Guo DeXiang.,Liu YaJing.,Li Ting.,Wang Nan.,Zhai Xin.,...&Gong Ping.(2012).Synthesis and antitumor activities of a new series of 4,5-dihydro-1H-thiochromeno4,3-dpyrimidine derivatives.SCIENCE CHINA-CHEMISTRY,55(3),347-351. |
MLA | Guo DeXiang,et al."Synthesis and antitumor activities of a new series of 4,5-dihydro-1H-thiochromeno4,3-dpyrimidine derivatives".SCIENCE CHINA-CHEMISTRY 55.3(2012):347-351. |
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