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Synthesis and antitumor activities of a new series of 4,5-dihydro-1H-thiochromeno4,3-dpyrimidine derivatives
Alternative TitleSynthesis 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 PublicationSCIENCE CHINA-CHEMISTRY
ISSN1674-7291
Volume55Issue:3Pages:347-351
AbstractA 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 AbstractA 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.
Keywordheterocycle synthesis 4,5-dihydro-1H-thiochromeno4,3-dpyrimidine derivatives antitumor activity
Indexed ByCSCD
Language英语
Funding Project[National Natural Science Foundation of China]
CSCD IDCSCD:4537942
Citation statistics
Document Type期刊论文
Identifierhttp://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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