Anti HIV-1 agents 5: Synthesis and anti-HIV-1 activity of some N-arylsulfonyl-3-acetylindoles in vitro

	Anti HIV-1 agents 5: Synthesis and anti-HIV-1 activity of some N-arylsulfonyl-3-acetylindoles in vitro
	Ran JQ 1; Huang N 2; Xu H[]1; Yang LM 2; Lv M[]1; Zheng YT[*]2; orgxuhui@nwsuaf.edu.cn ; lvmin@nwsuaf.edu.cn ; zhengyt@mail.kiz.ac.cn
	2010
发表期刊	BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN	0960-894X
卷号	20 期号:12 页码:3534-3536
合作性质	其它
摘要	In continuation of our program aimed at the discovery and development of compounds with superior anti-human immunodeficiency virus type 1 (HIV-1) activity, 21N-arylsulfonyl-3-acetylindole analogs (2a-u) were synthesized and preliminarily evaluated as HIV-1 inhibitors in vitro. Among of all the analogs, several compounds exhibited significant anti-HIV-1 activity, especially N-phenylsulfonyl-3-acetyl-6-methylindole (2j) and N-(p-ethyl)phenylsulfonyl-3-acetyl-6-methylindole (2n) showed the most potent anti-HIV-1 activity with EC(50) values of 0.36 and 0.13 mu g/mL, and TI values of >555.55 and 791.85, respectively. It demonstrated that introduction of the acetyl group at the 3-position of N-arylsulfonyl-6-methylindoles could generally lead to the more potent analogs.
关键词	N-arylsulfonyl-3-acetylindole Acquired Immune-deficiency Syndrome Human Immunodeficiency Virus-1 Inhibitor
资助者	This study was supported by National Science Foundation of China (NSFC 30870825, 30530270, 30670669 and 30770700). The author gratefully acknowledges the support of K.C. Wong Education Foundation, Hong Kong. ; This study was supported by National Science Foundation of China (NSFC 30870825, 30530270, 30670669 and 30770700). The author gratefully acknowledges the support of K.C. Wong Education Foundation, Hong Kong. ; This study was supported by National Science Foundation of China (NSFC 30870825, 30530270, 30670669 and 30770700). The author gratefully acknowledges the support of K.C. Wong Education Foundation, Hong Kong. ; This study was supported by National Science Foundation of China (NSFC 30870825, 30530270, 30670669 and 30770700). The author gratefully acknowledges the support of K.C. Wong Education Foundation, Hong Kong.
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收录类别	其他
语种	英语
资助者	This study was supported by National Science Foundation of China (NSFC 30870825, 30530270, 30670669 and 30770700). The author gratefully acknowledges the support of K.C. Wong Education Foundation, Hong Kong. ; This study was supported by National Science Foundation of China (NSFC 30870825, 30530270, 30670669 and 30770700). The author gratefully acknowledges the support of K.C. Wong Education Foundation, Hong Kong. ; This study was supported by National Science Foundation of China (NSFC 30870825, 30530270, 30670669 and 30770700). The author gratefully acknowledges the support of K.C. Wong Education Foundation, Hong Kong. ; This study was supported by National Science Foundation of China (NSFC 30870825, 30530270, 30670669 and 30770700). The author gratefully acknowledges the support of K.C. Wong Education Foundation, Hong Kong.
文献类型	期刊论文
条目标识符	http://ir.kiz.ac.cn/handle/152453/4693
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; lvmin@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 712100, 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 650223, China
推荐引用方式 GB/T 7714	Ran JQ,Huang N,Xu H[*],et al. Anti HIV-1 agents 5: Synthesis and anti-HIV-1 activity of some N-arylsulfonyl-3-acetylindoles in vitro[J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,2010,20(12):3534-3536.
APA	Ran JQ.,Huang N.,Xu H[].,Yang LM.,Lv M[].,...&zhengyt@mail.kiz.ac.cn.(2010).Anti HIV-1 agents 5: Synthesis and anti-HIV-1 activity of some N-arylsulfonyl-3-acetylindoles in vitro.BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,20(12),3534-3536.
MLA	Ran JQ,et al."Anti HIV-1 agents 5: Synthesis and anti-HIV-1 activity of some N-arylsulfonyl-3-acetylindoles in vitro".BIOORGANIC & MEDICINAL CHEMISTRY LETTERS 20.12(2010):3534-3536.

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