Structural modifications of quinolone-3-carboxylic acids with anti-HIV activity

	Structural modifications of quinolone-3-carboxylic acids with anti-HIV activity
	He QQ 1; Gu SX 1; Liu J 2; Wu HQ 1; Zhang X 3; Yang LM 3; Zheng YT 3; Chen FE*1,4; rfchen@fudan.edu.cn
	2011
发表期刊	BIOORGANIC & MEDICINAL CHEMISTRY
卷号	19 期号:16 页码:5039-5045
合作性质	其它
摘要	A series of new quinolone-3-carboxylic acids featuring a hydroxyl group at C-5 position were synthesized and evaluated for their in vitro activity against HIV in C8166 cell culture. All the compounds showed anti-HIV-1 activity with low micromolar to submicromolar EC(50) values. The most active compound 2k exhibited activity against wild-type HIV-1 with an EC(50) value of 0.13 mu M. Preliminary structure-activity relationship of the newly synthesized quinolone analogues was also investigated. Further docking study revealed that the anti-HIV activity of these compounds might involve a two-metal chelating mechanism.
关键词	Hiv Integrase Inhibitor Quinolone-3-carboxylic Acids Two-metal Chelating Mechanism
资助者	This project was funded by China Postdoctoral Science Founda- tion (20100470625). The work was also supported in part by grant 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 Re- search Program of China (2009CB5223006). ; This project was funded by China Postdoctoral Science Founda- tion (20100470625). The work was also supported in part by grant 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 Re- search Program of China (2009CB5223006). ; This project was funded by China Postdoctoral Science Founda- tion (20100470625). The work was also supported in part by grant 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 Re- search Program of China (2009CB5223006). ; This project was funded by China Postdoctoral Science Founda- tion (20100470625). The work was also supported in part by grant 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 Re- search 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 (20100470625). The work was also supported in part by grant 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 Re- search Program of China (2009CB5223006). ; This project was funded by China Postdoctoral Science Founda- tion (20100470625). The work was also supported in part by grant 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 Re- search Program of China (2009CB5223006). ; This project was funded by China Postdoctoral Science Founda- tion (20100470625). The work was also supported in part by grant 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 Re- search Program of China (2009CB5223006). ; This project was funded by China Postdoctoral Science Founda- tion (20100470625). The work was also supported in part by grant 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 Re- search Program of China (2009CB5223006).
文献类型	期刊论文
条目标识符	http://ir.kiz.ac.cn/handle/353002/6711
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.Department of Medicinal Chemistry, School of Pharmacy, Second Millitary Medical University, Shanghai 200433, PR China 3.Key Laboratory of Animal Models and Human Disease Mechanisms of Chinese Academy of Sciences & Yunnan Province, Kunming Institute of Zoology, Chinese Academy of Sciences, Kunming 650223, PR China 4.Institute of Biomedical Science, Fudan University, Shanghai 200433, PR China
推荐引用方式 GB/T 7714	He QQ,Gu SX,Liu J,et al. Structural modifications of quinolone-3-carboxylic acids with anti-HIV activity[J]. BIOORGANIC & MEDICINAL CHEMISTRY,2011,19(16):5039-5045.
APA	He QQ.,Gu SX.,Liu J.,Wu HQ.,Zhang X.,...&rfchen@fudan.edu.cn.(2011).Structural modifications of quinolone-3-carboxylic acids with anti-HIV activity.BIOORGANIC & MEDICINAL CHEMISTRY,19(16),5039-5045.
MLA	He QQ,et al."Structural modifications of quinolone-3-carboxylic acids with anti-HIV activity".BIOORGANIC & MEDICINAL CHEMISTRY 19.16(2011):5039-5045.

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