Discovery of Novel Tricyclic 5H-Pyridazino4,5-bindoles as Potent Antitumor Agents: Design, Synthesis and Biological Evaluation

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	Discovery of Novel Tricyclic 5H-Pyridazino4,5-bindoles as Potent Antitumor Agents: Design, Synthesis and Biological Evaluation
其他题名	Discovery of Novel Tricyclic 5H-Pyridazino4,5-bindoles as Potent Antitumor Agents: Design,Synthesis and Biological Evaluation
	Zhai Xin; Wang Limei; Shi Jiyue; Gong Ping
	2015
发表期刊	CHEMICAL RESEARCH IN CHINESE UNIVERSITIES
ISSN	1005-9040
卷号	31 期号:3 页码:372-380
摘要	A novel series of 5H-pyridazino4,5-bindoles(L-01-L-32) was synthesized and characterized by means of H-1 NMR, MS and elemental analysis. The cytotoxicity of the target compounds against Bel-7402 and HT-1080 cell lines were evaluated by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide(MTT) assay. Most of them exhibited moderate to excellent cytotoxicity, and six compounds(L-04, L-06, L-18, L-20, L-21 and L-23) possessed dramatically increased cytotoxicity superior to Gefitinib. Of these initial hits, compound L-21 displayed remarkable cytotoxicity against the tested cell lines with half maximal inhibitory concentration(IC50) values of 4.6 and 2.1 mu mol/L, respectively, which was 13.9- to 25.6-fold more potent than positive control.
其他摘要	A novel series of 5H-pyridazino4,5-bindoles(L-01-L-32) was synthesized and characterized by means of ~1H NMR, MS and elemental analysis. The cytotoxicity of the target compounds against Bel-7402 and HT-1080 cell lines were evaluated by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide(MTT) assay. Most of them exhibited moderate to excellent cytotoxicity, and six compounds(L-04, L-06, L-18, L-20, L-21 and L-23) possessed dramatically increased cytotoxicity superior to Gefitinib. Of these initial hits, compound L-21 displayed remarkable cytotoxicity against the tested cell lines with half maximal inhibitory concentration(IC_(50)) values of 4.6 and 2.1 μmol/L, respectively, which was 13.9- to 25.6-fold more potent than positive control.
关键词	TYROSINE KINASE INHIBITORS GROWTH-FACTOR RECEPTOR ANALOGS DERIVATIVES BINDING HARMINE 1-Anilino-5H-pyridazino4,5-bindole EGFR inhibitor Cytotoxicity
收录类别	CSCD
语种	英语
资助项目	[National Natural Science Foundation of China] ; [Liaoning Baiqianwan Talents Program, China]
CSCD记录号	CSCD:5434854
引用统计	被引频次：2[CSCD] [CSCD记录]
文献类型	期刊论文
条目标识符	http://ir.imr.ac.cn/handle/321006/150263
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,Wang Limei,Shi Jiyue,et al. Discovery of Novel Tricyclic 5H-Pyridazino4,5-bindoles as Potent Antitumor Agents: Design, Synthesis and Biological Evaluation[J]. CHEMICAL RESEARCH IN CHINESE UNIVERSITIES,2015,31(3):372-380.
APA	Zhai Xin,Wang Limei,Shi Jiyue,&Gong Ping.(2015).Discovery of Novel Tricyclic 5H-Pyridazino4,5-bindoles as Potent Antitumor Agents: Design, Synthesis and Biological Evaluation.CHEMICAL RESEARCH IN CHINESE UNIVERSITIES,31(3),372-380.
MLA	Zhai Xin,et al."Discovery of Novel Tricyclic 5H-Pyridazino4,5-bindoles as Potent Antitumor Agents: Design, Synthesis and Biological Evaluation".CHEMICAL RESEARCH IN CHINESE UNIVERSITIES 31.3(2015):372-380.