Syntheses and Antiproliferative Activities of Novel Diarylthiosemicarbazide Derivatives

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	Syntheses and Antiproliferative Activities of Novel Diarylthiosemicarbazide Derivatives
其他题名	Syntheses and Antiproliferative Activities of Novel Diarylthiosemicarbazide Derivatives
	Zhai Xin; He Ying; Yang Zhen; Gong Ping
	2013
发表期刊	CHEMICAL RESEARCH IN CHINESE UNIVERSITIES
ISSN	1005-9040
卷号	29 期号:1 页码:62-66
摘要	A series of novel N-methylpicolinamide-moiety containing diarylthiosemicarbazide derivatives was prepared and evaluated for their in vitro antiproliferative activity against three cancer cell lines(human alveolar epithelial cell A549, human lung cancer cell 11460 and human colorectal cancer cell HT-29) by 3-(4,5-dimethyl)thiazolyl-diphenyltetrazoliumromide(MTT) assay. Six compounds(7b-7g) with halogen substituents exhibited preferable cytotoxicity against one or more cell lines in a low micromolar range. Especially, the most promising compound 7g exhibited remarkable antiproliferative activity with the IC50 values of 2.2, 1.8 and 5.2 mu mol/L against A549, 11460 and HT-29 cell lines respectively, which is comparable to sorafenib.
其他摘要	A series of novel N-methylpicolinamide-moiety containing diarylthiosemicarbazide derivatives was prepared and evaluated for their in vitro antiproliferative activity against three cancer cell lines(human alveolar epithelial cell A549,human lung cancer cell H460 and human colorectal cancer cell HT-29) by 3-(4,5-dimethyl)thiazolyl- diphenyltetrazoliumromide(MTT) assay. Six compounds(7b―7g) with halogen substituents exhibited preferable cytotoxicity against one or more cell lines in a low micromolar range. Especially,the most promising compound 7g exhibited remarkable antiproliferative activity with the IC50 values of 2.2,1.8 and 5.2 μmol/L against A549,H460 and HT-29 cell lines respectively,which is comparable to sorafenib.
关键词	KINASE INHIBITORS ANTITUMOR AGENTS DESIGN BENZIMIDAZOLES CYTOTOXICITY Thiosemicarbazide N-methylpicolinamide Antiproliferative activity
收录类别	CSCD
语种	英语
资助项目	[National Natural Science Foundation of China] ; [Science & Technology Project of Liaoning Province, China]
CSCD记录号	CSCD:4756394
引用统计	被引频次：4[CSCD] [CSCD记录]
文献类型	期刊论文
条目标识符	http://ir.imr.ac.cn/handle/321006/146988
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	Zhai Xin,He Ying,Yang Zhen,et al. Syntheses and Antiproliferative Activities of Novel Diarylthiosemicarbazide Derivatives[J]. CHEMICAL RESEARCH IN CHINESE UNIVERSITIES,2013,29(1):62-66.
APA	Zhai Xin,He Ying,Yang Zhen,&Gong Ping.(2013).Syntheses and Antiproliferative Activities of Novel Diarylthiosemicarbazide Derivatives.CHEMICAL RESEARCH IN CHINESE UNIVERSITIES,29(1),62-66.
MLA	Zhai Xin,et al."Syntheses and Antiproliferative Activities of Novel Diarylthiosemicarbazide Derivatives".CHEMICAL RESEARCH IN CHINESE UNIVERSITIES 29.1(2013):62-66.