Synthesis and biological evaluation of HQCAs with aryl or benzyl substituents on N-1 position as potential HIV-1 integrase inhibitors

	Synthesis and biological evaluation of HQCAs with aryl or benzyl substituents on N-1 position as potential HIV-1 integrase inhibitors
	He QQ 1; Zhang X 2; Wu HQ 1; Gu SX 1; Ma XD 1; Yang LM 2; Zheng YT 2; Chen FE[*]1,3; rfchen@fudan.edu.cn
	2011
发表期刊	BIOORGANIC & MEDICINAL CHEMISTRY
卷号	19 期号:18 页码:5553-5558
合作性质	其它
摘要	A series of new 5-hydroxylquinolone-3-carboxylic acids (HQCAs) with various aryl or benzyl substituents on N-1 position were synthesized and evaluated for their anti-HIV activity in C8166 cell culture. Most of the target compounds displayed activity against wide-type HIV-1 in the low micromolar range in infected C8166 cells. The most active compound 5g exhibited activity against wild-type HIV-1 and HIV-1 mutant virus A17 with an EC(50) value of 3.17 and 17.88 mu M, respectively. The biological results and the docking study revealed that the substitution pattern on N-1 position of the quinolone core might contribute to physicochemical properties of HQCAs and resulted in great influence on their antiviral potency.
关键词	Hiv Integrase Inhibitor Quinolone-3-carboxylic Acids Two-metal Chelating Mechanism Structure-activity Relationships
资助者	This project was funded by China Postdoctoral Science Founda- tion(20100470624). The work was also supported in part by grants from the National Natural Science Foundation of China(20872018), from Chinese Academy of Sciences (KSCX2-YW-R-185), from the Eleventh Five-Year Key Scientific and Technological Program of China (2009ZX09501-029), and from National Basic Research Program of China (2009CB5223006). ; This project was funded by China Postdoctoral Science Founda- tion(20100470624). The work was also supported in part by grants from the National Natural Science Foundation of China(20872018), from Chinese Academy of Sciences (KSCX2-YW-R-185), from the Eleventh Five-Year Key Scientific and Technological Program of China (2009ZX09501-029), and from National Basic Research Program of China (2009CB5223006). ; This project was funded by China Postdoctoral Science Founda- tion(20100470624). The work was also supported in part by grants from the National Natural Science Foundation of China(20872018), from Chinese Academy of Sciences (KSCX2-YW-R-185), from the Eleventh Five-Year Key Scientific and Technological Program of China (2009ZX09501-029), and from National Basic Research Program of China (2009CB5223006). ; This project was funded by China Postdoctoral Science Founda- tion(20100470624). The work was also supported in part by grants from the National Natural Science Foundation of China(20872018), from Chinese Academy of Sciences (KSCX2-YW-R-185), from the Eleventh Five-Year Key Scientific and Technological Program of China (2009ZX09501-029), and from National Basic Research Program of China (2009CB5223006).
收录类别	SCI
语种	英语
资助者	This project was funded by China Postdoctoral Science Founda- tion(20100470624). The work was also supported in part by grants from the National Natural Science Foundation of China(20872018), from Chinese Academy of Sciences (KSCX2-YW-R-185), from the Eleventh Five-Year Key Scientific and Technological Program of China (2009ZX09501-029), and from National Basic Research Program of China (2009CB5223006). ; This project was funded by China Postdoctoral Science Founda- tion(20100470624). The work was also supported in part by grants from the National Natural Science Foundation of China(20872018), from Chinese Academy of Sciences (KSCX2-YW-R-185), from the Eleventh Five-Year Key Scientific and Technological Program of China (2009ZX09501-029), and from National Basic Research Program of China (2009CB5223006). ; This project was funded by China Postdoctoral Science Founda- tion(20100470624). The work was also supported in part by grants from the National Natural Science Foundation of China(20872018), from Chinese Academy of Sciences (KSCX2-YW-R-185), from the Eleventh Five-Year Key Scientific and Technological Program of China (2009ZX09501-029), and from National Basic Research Program of China (2009CB5223006). ; This project was funded by China Postdoctoral Science Founda- tion(20100470624). The work was also supported in part by grants from the National Natural Science Foundation of China(20872018), from Chinese Academy of Sciences (KSCX2-YW-R-185), from the Eleventh Five-Year Key Scientific and Technological Program of China (2009ZX09501-029), and from National Basic Research Program of China (2009CB5223006).
文献类型	期刊论文
条目标识符	http://ir.kiz.ac.cn/handle/353002/6810
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	rfchen@fudan.edu.cn
作者单位	1.Department of Chemistry, Fudan University, Shanghai 200433, PR China 2.Key Laboratory of Animal Models and Human Disease Mechanisms of Chinese Academy of Sciences and Yunnan Province, Kunming Institute of Zoology, Chinese Academy of Sciences, Kunming 650223, PR China 3.Institute of Biomedical Science, Fudan University, Shanghai 200433, PR China
推荐引用方式 GB/T 7714	He QQ,Zhang X,Wu HQ,et al. Synthesis and biological evaluation of HQCAs with aryl or benzyl substituents on N-1 position as potential HIV-1 integrase inhibitors[J]. BIOORGANIC & MEDICINAL CHEMISTRY,2011,19(18):5553-5558.
APA	He QQ.,Zhang X.,Wu HQ.,Gu SX.,Ma XD.,...&rfchen@fudan.edu.cn.(2011).Synthesis and biological evaluation of HQCAs with aryl or benzyl substituents on N-1 position as potential HIV-1 integrase inhibitors.BIOORGANIC & MEDICINAL CHEMISTRY,19(18),5553-5558.
MLA	He QQ,et al."Synthesis and biological evaluation of HQCAs with aryl or benzyl substituents on N-1 position as potential HIV-1 integrase inhibitors".BIOORGANIC & MEDICINAL CHEMISTRY 19.18(2011):5553-5558.

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