Synthesis and biological evaluation of novel amprenavir-based P1-substituted bi-aryl derivatives as ultra-potent HIV-1 protease inhibitors

CORC > 昆明动物研究所 > 昆明动物研究所 > 动物模型与人类重大疾病机理重点实验室 > 分子免疫药理学

	Synthesis and biological evaluation of novel amprenavir-based P1-substituted bi-aryl derivatives as ultra-potent HIV-1 protease inhibitors
	Yan JW 1; Huang N 2; Li SK 1; Yang LM 2; Xing WQ 1; Zheng YT[]2; Hu YH[]1
刊名	BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
	2012
卷号	22 期号:5 页码:1976-1979
关键词	HIV-1 protease inhibitors Amprenavir Darunavir biaryl compounds Docking study
通讯作者	zhengyt@mail.kiz.ac.cn ; yhhu@mail.shcnc.ac.cn
合作状况	其它
英文摘要	A series of P1-substituted biaryl amprenavir derivatives was designed and synthesized. These compounds were evaluated for enzyme inhibition and antiviral activity in vitro. Several compounds showed highly efficient antiviral activity with EC50 values down to 0.10 nM, which are more potent than marketed HIV-1 protease inhibitors. Docking study indicated that 12c has similar binding mode to amprenavir with full occupancy in P1.
收录类别	SCI
资助信息	This work was supported by the National Natural Science Foun- dation of China (Grant Nos.: 30600775, 81001462), the Eleventh Five-Year Key Scientific and Technological Program of China (2009ZX09501-029) and the CAS Knowledge Innovation Project (KSCX2-YW-R-185).
语种	英语
WOS记录号	WOS:000300451200028
公开日期	2012-03-19
内容类型	期刊论文
源URL	[http://159.226.149.42:8088/handle/353002/6873]
专题	昆明动物研究所_分子免疫药理学昆明动物研究所_动物模型与人类重大疾病机理重点实验室
作者单位	1.State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, 555 Zu Chong Zhi Road, Shanghai 201203, China 2.Key Laboratory of Animal Models and Human Disease Mechanisms of the Chinese Academy of Science & YunnanProvince, Kunming Institute of Zoology, Chinese Academy of Sciences, Kunming, Yunnan 650223, China
推荐引用方式 GB/T 7714	Yan JW,Huang N,Li SK,et al. Synthesis and biological evaluation of novel amprenavir-based P1-substituted bi-aryl derivatives as ultra-potent HIV-1 protease inhibitors[J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,2012,22(5):1976-1979.
APA	Yan JW.,Huang N.,Li SK.,Yang LM.,Xing WQ.,...&Hu YH[*].(2012).Synthesis and biological evaluation of novel amprenavir-based P1-substituted bi-aryl derivatives as ultra-potent HIV-1 protease inhibitors.BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,22(5),1976-1979.
MLA	Yan JW,et al."Synthesis and biological evaluation of novel amprenavir-based P1-substituted bi-aryl derivatives as ultra-potent HIV-1 protease inhibitors".BIOORGANIC & MEDICINAL CHEMISTRY LETTERS 22.5(2012):1976-1979.