Synthesis of New 2-(N-Arylsulfonylindol-3-yl)-3-aryl-1,3-thiazolidin-4-ones as HIV-1 Inhibitors In Vitro

	Synthesis of New 2-(N-Arylsulfonylindol-3-yl)-3-aryl-1,3-thiazolidin-4-ones as HIV-1 Inhibitors In Vitro
	Yang RG 1; Yang LM 2; Ke YZ 1; Huang N 2,3; Zhang R 1; Zheng YT2; Xu H1; orgxuhui@nwsuaf.edu.cn, zhengyt@mail.kiz.ac.cn
	2012
发表期刊	LETTERS IN DRUG DESIGN & DISCOVERY
卷号	9 期号:4 页码:415-420
合作性质	其它
摘要	Twenty-one 2-(N-arylsulfonylindol-3-yl)-3-aryl-1,3-thiazolidin-4-ones (4a-u) were synthesized and evaluated as HIV-1 inhibitors in vitro. Among all compounds, compounds 4n and 4p displayed the potent anti-HIV-1 activities with EC50 values of 3.48 and 8.61 mu g/mL, and TI values of 34.08 and > 23.22, respectively. It demonstrated that, to a series of 2-(N-arylsulfonyl-6-methylindol-3-yl)-3-aryl-1,3-thiazolidin-4-one derivatives, introduction of R-2 as 4-Cl and R-3 as H or 3-Cl could afford the more promising and potent compounds.
关键词	Acquired Immunodeficiency Syndrome 2-(N-arylsulfonylindol-3-yl)-3-aryl-1 Human Immunodeficiency Virus-1 3-thiazolidin-4-ones Aids
资助者	This work has been supported by the Special Funds of Central Colleges Basic Scientific Research Operating Expenses (QN2009045), and the Science & Technology Research Plan in Shaanxi province of China (2010K02-09- 3). We also would like to acknowledge the National Basic Research Program of China (2009CB522306), National Natural Science Foundation of China (81102483), Eleventh Five-Year Key Scientific and Technological Program of China (2009ZX09501-029) and the MRC AIDS Research Project and the NIH AIDS Research and Reference Reagent Program for providing cell lines and viruses. ; This work has been supported by the Special Funds of Central Colleges Basic Scientific Research Operating Expenses (QN2009045), and the Science & Technology Research Plan in Shaanxi province of China (2010K02-09- 3). We also would like to acknowledge the National Basic Research Program of China (2009CB522306), National Natural Science Foundation of China (81102483), Eleventh Five-Year Key Scientific and Technological Program of China (2009ZX09501-029) and the MRC AIDS Research Project and the NIH AIDS Research and Reference Reagent Program for providing cell lines and viruses. ; This work has been supported by the Special Funds of Central Colleges Basic Scientific Research Operating Expenses (QN2009045), and the Science & Technology Research Plan in Shaanxi province of China (2010K02-09- 3). We also would like to acknowledge the National Basic Research Program of China (2009CB522306), National Natural Science Foundation of China (81102483), Eleventh Five-Year Key Scientific and Technological Program of China (2009ZX09501-029) and the MRC AIDS Research Project and the NIH AIDS Research and Reference Reagent Program for providing cell lines and viruses. ; This work has been supported by the Special Funds of Central Colleges Basic Scientific Research Operating Expenses (QN2009045), and the Science & Technology Research Plan in Shaanxi province of China (2010K02-09- 3). We also would like to acknowledge the National Basic Research Program of China (2009CB522306), National Natural Science Foundation of China (81102483), Eleventh Five-Year Key Scientific and Technological Program of China (2009ZX09501-029) and the MRC AIDS Research Project and the NIH AIDS Research and Reference Reagent Program for providing cell lines and viruses.
收录类别	SCI
语种	英语
资助者	This work has been supported by the Special Funds of Central Colleges Basic Scientific Research Operating Expenses (QN2009045), and the Science & Technology Research Plan in Shaanxi province of China (2010K02-09- 3). We also would like to acknowledge the National Basic Research Program of China (2009CB522306), National Natural Science Foundation of China (81102483), Eleventh Five-Year Key Scientific and Technological Program of China (2009ZX09501-029) and the MRC AIDS Research Project and the NIH AIDS Research and Reference Reagent Program for providing cell lines and viruses. ; This work has been supported by the Special Funds of Central Colleges Basic Scientific Research Operating Expenses (QN2009045), and the Science & Technology Research Plan in Shaanxi province of China (2010K02-09- 3). We also would like to acknowledge the National Basic Research Program of China (2009CB522306), National Natural Science Foundation of China (81102483), Eleventh Five-Year Key Scientific and Technological Program of China (2009ZX09501-029) and the MRC AIDS Research Project and the NIH AIDS Research and Reference Reagent Program for providing cell lines and viruses. ; This work has been supported by the Special Funds of Central Colleges Basic Scientific Research Operating Expenses (QN2009045), and the Science & Technology Research Plan in Shaanxi province of China (2010K02-09- 3). We also would like to acknowledge the National Basic Research Program of China (2009CB522306), National Natural Science Foundation of China (81102483), Eleventh Five-Year Key Scientific and Technological Program of China (2009ZX09501-029) and the MRC AIDS Research Project and the NIH AIDS Research and Reference Reagent Program for providing cell lines and viruses. ; This work has been supported by the Special Funds of Central Colleges Basic Scientific Research Operating Expenses (QN2009045), and the Science & Technology Research Plan in Shaanxi province of China (2010K02-09- 3). We also would like to acknowledge the National Basic Research Program of China (2009CB522306), National Natural Science Foundation of China (81102483), Eleventh Five-Year Key Scientific and Technological Program of China (2009ZX09501-029) and the MRC AIDS Research Project and the NIH AIDS Research and Reference Reagent Program for providing cell lines and viruses.
文献类型	期刊论文
条目标识符	http://ir.kiz.ac.cn/handle/152453/6957
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 Design & Synthesis, College of Sciences, Northwest A&F University, Yangling, Shaanxi 712100, P. R. China 2.Key Laboratory of Animal Models and Human Diseases Mechanisms of Chinese Academy of Sciences and Yunnan Province, Kunming Institute of Zoology, Chinese Academy of Sciences, Kunming, Yunnan 650223, P. R. China 3.Graduate School of the Chinese Academy of Sciences, Beijing 100039, China
推荐引用方式 GB/T 7714	Yang RG,Yang LM,Ke YZ,et al. Synthesis of New 2-(N-Arylsulfonylindol-3-yl)-3-aryl-1,3-thiazolidin-4-ones as HIV-1 Inhibitors In Vitro[J]. LETTERS IN DRUG DESIGN & DISCOVERY,2012,9(4):415-420.
APA	Yang RG.,Yang LM.,Ke YZ.,Huang N.,Zhang R.,...&orgxuhui@nwsuaf.edu.cn, zhengyt@mail.kiz.ac.cn.(2012).Synthesis of New 2-(N-Arylsulfonylindol-3-yl)-3-aryl-1,3-thiazolidin-4-ones as HIV-1 Inhibitors In Vitro.LETTERS IN DRUG DESIGN & DISCOVERY,9(4),415-420.
MLA	Yang RG,et al."Synthesis of New 2-(N-Arylsulfonylindol-3-yl)-3-aryl-1,3-thiazolidin-4-ones as HIV-1 Inhibitors In Vitro".LETTERS IN DRUG DESIGN & DISCOVERY 9.4(2012):415-420.

条目包含的文件
文件名称/大小	文献类型	版本类型	开放类型	使用许可
2012053107.pdf（223KB）	期刊论文	出版稿	开放获取	CC BY-NC-SA	请求全文