Synthesis and HIV-1 integrase inhibition activity of some N-arylindoles

	Synthesis and HIV-1 integrase inhibition activity of some N-arylindoles
	Xu H1; Liu WQ 2; Fan LL 1; Chen Y 1; Yang LM 2; Lv L 1; Zheng YT2; orgxuhui@nwsuaf.edu.cn ; zhengyt@mail.kiz.ac.cn
	2008
发表期刊	CHEMICAL & PHARMACEUTICAL BULLETIN
ISSN	0009-2363
卷号	56 期号:5 页码:720-722
合作性质	其它
摘要	Eight simple N-arylindoles were designed, synthesized and evaluated as human immunodeficiency virus (HIV)-1 integrase inhibitors in vitro for the first time. Among these compounds, 3b, 3e and 3g demonstrated significant anti-HIV-1 integrase activity. Especially 3b showed the highest anti-HIV-1 integrase activity with EC50 value of 7.88 mu g/ml and TI value of 24.61. Meantime, some structure-activity relationships were also observed and will provide a new lead for design and discovery of more potent N-arylindoles as HIV-1 integrase inhibitors.
关键词	N-arylindole Anti-human Immunodeficiency Virus Type 1 Integrase Inhibitor Synthesis
资助者	This work has been supported by the program for New Century Excellent University Talents (NCET-06-0868), State Educa- tion Ministry of China, and the Science & Technology Research Plan in Shaanxi Province of China (No. 2006K01-G31-04). We also would like to acknowledge Key Scientific and Technological Projects of Yunnan province (2004NG12), National 973 project of China (2006CB504200), The Knowl- edge Innovation Program of CAS (KSCX1-YW-R-24). ; This work has been supported by the program for New Century Excellent University Talents (NCET-06-0868), State Educa- tion Ministry of China, and the Science & Technology Research Plan in Shaanxi Province of China (No. 2006K01-G31-04). We also would like to acknowledge Key Scientific and Technological Projects of Yunnan province (2004NG12), National 973 project of China (2006CB504200), The Knowl- edge Innovation Program of CAS (KSCX1-YW-R-24). ; This work has been supported by the program for New Century Excellent University Talents (NCET-06-0868), State Educa- tion Ministry of China, and the Science & Technology Research Plan in Shaanxi Province of China (No. 2006K01-G31-04). We also would like to acknowledge Key Scientific and Technological Projects of Yunnan province (2004NG12), National 973 project of China (2006CB504200), The Knowl- edge Innovation Program of CAS (KSCX1-YW-R-24). ; This work has been supported by the program for New Century Excellent University Talents (NCET-06-0868), State Educa- tion Ministry of China, and the Science & Technology Research Plan in Shaanxi Province of China (No. 2006K01-G31-04). We also would like to acknowledge Key Scientific and Technological Projects of Yunnan province (2004NG12), National 973 project of China (2006CB504200), The Knowl- edge Innovation Program of CAS (KSCX1-YW-R-24).
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收录类别	SCI
语种	英语
资助者	This work has been supported by the program for New Century Excellent University Talents (NCET-06-0868), State Educa- tion Ministry of China, and the Science & Technology Research Plan in Shaanxi Province of China (No. 2006K01-G31-04). We also would like to acknowledge Key Scientific and Technological Projects of Yunnan province (2004NG12), National 973 project of China (2006CB504200), The Knowl- edge Innovation Program of CAS (KSCX1-YW-R-24). ; This work has been supported by the program for New Century Excellent University Talents (NCET-06-0868), State Educa- tion Ministry of China, and the Science & Technology Research Plan in Shaanxi Province of China (No. 2006K01-G31-04). We also would like to acknowledge Key Scientific and Technological Projects of Yunnan province (2004NG12), National 973 project of China (2006CB504200), The Knowl- edge Innovation Program of CAS (KSCX1-YW-R-24). ; This work has been supported by the program for New Century Excellent University Talents (NCET-06-0868), State Educa- tion Ministry of China, and the Science & Technology Research Plan in Shaanxi Province of China (No. 2006K01-G31-04). We also would like to acknowledge Key Scientific and Technological Projects of Yunnan province (2004NG12), National 973 project of China (2006CB504200), The Knowl- edge Innovation Program of CAS (KSCX1-YW-R-24). ; This work has been supported by the program for New Century Excellent University Talents (NCET-06-0868), State Educa- tion Ministry of China, and the Science & Technology Research Plan in Shaanxi Province of China (No. 2006K01-G31-04). We also would like to acknowledge Key Scientific and Technological Projects of Yunnan province (2004NG12), National 973 project of China (2006CB504200), The Knowl- edge Innovation Program of CAS (KSCX1-YW-R-24).
文献类型	期刊论文
条目标识符	http://ir.kiz.ac.cn/handle/152453/4639
专题	科研部门_分子免疫药理学（郑永唐）科研部门_动物模型与人类重大疾病机理重点实验室
通讯作者	orgxuhui@nwsuaf.edu.cn; zhengyt@mail.kiz.ac.cn
作者单位	1.Laboratory of Pharmaceutical Synthesis, College of Sciences, Northwest A&F University; Yangling 712100, China 2.Laboratory of Molecular Immunopharmacology, Key Laboratory of Animal Models and Human Diseases Mechanisms, Kunming Institute of Zoology, Chinese Academy of Sciences; Kunming 650223, China
推荐引用方式 GB/T 7714	Xu H*,Liu WQ,Fan LL,et al. Synthesis and HIV-1 integrase inhibition activity of some N-arylindoles[J]. CHEMICAL & PHARMACEUTICAL BULLETIN,2008,56(5):720-722.
APA	Xu H*.,Liu WQ.,Fan LL.,Chen Y.,Yang LM.,...&zhengyt@mail.kiz.ac.cn.(2008).Synthesis and HIV-1 integrase inhibition activity of some N-arylindoles.CHEMICAL & PHARMACEUTICAL BULLETIN,56(5),720-722.
MLA	Xu H*,et al."Synthesis and HIV-1 integrase inhibition activity of some N-arylindoles".CHEMICAL & PHARMACEUTICAL BULLETIN 56.5(2008):720-722.

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