Design, Synthesis and Anticancer Activity of Novel 6-(Aminophenyl)-2,4-bismorpholino-1,3,5-triazine Derivatives Bearing Arylmethylene Hydrazine Moiety

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	Design, Synthesis and Anticancer Activity of Novel 6-(Aminophenyl)-2,4-bismorpholino-1,3,5-triazine Derivatives Bearing Arylmethylene Hydrazine Moiety
其他题名	Design, Synthesis and Anticancer Activity of Novel 6-(Aminophenyl)-2,4-bismorpholino-1,3,5-triazine Derivatives Bearing Arylmethylene Hydrazine Moiety
	Huang Qiang; Fu Qiangqiang; Liu Yajing; Bai Jinying; Wang Qianying; Liao Huimin; Gong Ping
	2014
发表期刊	CHEMICAL RESEARCH IN CHINESE UNIVERSITIES
ISSN	1005-9040
卷号	30 期号:2 页码:257-265
摘要	In an attempt to develop potent and selective anticancer agents, we designed and synthesized a series of novel bis(morpholino-1,3,5-triazine) derivatives bearing aylmethylene hydrazine moiety and evaluated their cytotoxicity, in vitro, against H460(non-small-cell lung cancer), HT-29(human colorectal cancer) and MDA-MB-231(human breast cancer) cell lines. The pharmacological results indicate that all the compounds exhibit enhanced cytotoxicity than BMCL-200908069-1, and six target compounds(7e, 7h, 7j, 9a, 9b, 9c) were superior to PAC-1 against all the tested cancer cell lines. The most active compound 7j, with IC50(inhibitory concentration 50%) values of 0.75, 0.34 and 0.60 mu mol/L against HT-29, H460 and MDA-MB-231 cancer cell lines, was 39-, 28-, and 60-fold more potent than BMCL-200908069-1(29.24, 9.52 and 36.21 mu mol/L), respectively.
其他摘要	In an attempt to develop potent and selective anticancer agents, we designed and synthesized a series of novel bis(morpholino-1,3,5-triazine) derivatives bearing aylmethylene hydrazine moiety and evaluated their cytotoxicity, in vitro, against H460(non-small-cell lung cancer), HT-29(human colorectal cancer) and MDA-MB-231(human breast cancer) cell lines. The pharmacological results indicate that all the compounds exhibit enhanced cytotoxicity than BMCL-200908069-1, and six target compounds(7e, 7h, 7j, 9a, 9b, 9c) were superior to PAC-1 against all the tested cancer cell lines. The most active compound 7j, with IC_(50)(inhibitory concentration 50%) values of 0.75, 0.34 and 0.60 μmol/L against HT-29, H460 and MDA-MB-231 cancer cell lines, was 39-, 28-, and 60-fold more potent than BMCL-200908069-1(29.24, 9.52 and 36.21 μmol/L), respectively.
关键词	POTENTIAL ANTITUMOR AGENTS BIOLOGICAL EVALUATION INHIBITOR MTOR Bis(morpholino-1,3,5-triazine) Design Anticancer activity
收录类别	CSCD
语种	英语
资助项目	[Program for Innovative Research Team of the Ministry of Education] ; [Program for Liaoning Innovative Research Team in University, China]
CSCD记录号	CSCD:5111876
引用统计
文献类型	期刊论文
条目标识符	http://ir.imr.ac.cn/handle/321006/147503
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	Huang Qiang,Fu Qiangqiang,Liu Yajing,et al. Design, Synthesis and Anticancer Activity of Novel 6-(Aminophenyl)-2,4-bismorpholino-1,3,5-triazine Derivatives Bearing Arylmethylene Hydrazine Moiety[J]. CHEMICAL RESEARCH IN CHINESE UNIVERSITIES,2014,30(2):257-265.
APA	Huang Qiang.,Fu Qiangqiang.,Liu Yajing.,Bai Jinying.,Wang Qianying.,...&Gong Ping.(2014).Design, Synthesis and Anticancer Activity of Novel 6-(Aminophenyl)-2,4-bismorpholino-1,3,5-triazine Derivatives Bearing Arylmethylene Hydrazine Moiety.CHEMICAL RESEARCH IN CHINESE UNIVERSITIES,30(2),257-265.
MLA	Huang Qiang,et al."Design, Synthesis and Anticancer Activity of Novel 6-(Aminophenyl)-2,4-bismorpholino-1,3,5-triazine Derivatives Bearing Arylmethylene Hydrazine Moiety".CHEMICAL RESEARCH IN CHINESE UNIVERSITIES 30.2(2014):257-265.