Synthesis and antitumor activities of a new series of 4,5-dihydro-1H-thiochromeno4,3-dpyrimidine derivatives

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	Synthesis and antitumor activities of a new series of 4,5-dihydro-1H-thiochromeno4,3-dpyrimidine derivatives
其他题名	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
发表期刊	SCIENCE CHINA-CHEMISTRY
ISSN	1674-7291
卷号	55 期号:3 页码:347-351
摘要	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.
其他摘要	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.
关键词	heterocycle synthesis 4,5-dihydro-1H-thiochromeno4,3-dpyrimidine derivatives antitumor activity
收录类别	CSCD
语种	英语
资助项目	[National Natural Science Foundation of China]
CSCD记录号	CSCD:4537942
引用统计
文献类型	期刊论文
条目标识符	http://ir.imr.ac.cn/handle/321006/147775
专题	中国科学院金属研究所
作者单位	中国科学院金属研究所
推荐引用方式 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.