Synthesis and biological evaluation of novel dihydro-aryl/alkylsulfanyl-cyclohexylmethyl-oxopyrimidines (S-DACOs) as high active anti-HIV agents

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 dihydro-aryl/alkylsulfanyl-cyclohexylmethyl-oxopyrimidines (S-DACOs) as high active anti-HIV agents
	He YP[*]1; Long J 2; Zhang SS 1; Li C 1; Lai CC 3; Zhang CS 1; Li DX 1; Zhang DH 1; Wang H 1; Cai QQ 1
刊名	BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
	2011
卷号	21 期号:2 页码:694-697
关键词	NNRTIs S-DABOs S-DACOs Anti HIV-1 activity
通讯作者	yphe@ynu.edu.cn ; zhengyt@mail.kiz.ac.cn
合作状况	其它
英文摘要	A novel dihydro-aryl/alkylsulfanyl-cyclohexylmethyl-oxopyrimidines (S-DACOs) combinatory library was synthesized and evaluated with C8166 cells infected by the HIV-1(IIIB) in vitro, using Nevirapine (NVP) and Zidovudine (AZT) as positive control. The anti-HIV screening results revealed that C-6-cyclohexylmethyl substituted pyrimidinones possessed higher selective index than its 6-arylmethyl counterparts. Compounds 1g, 1c, 1e and 1b showed potent anti-HIV activities with EC50 values of 0.012, 0.025, 0.088 and 0.162 nM, respectively
收录类别	SCI
资助信息	This research was supported by the National Natural Science Foundation of China (Grant No. 30560179 and 30960459), the Sci- ence Foundation of Chinese academy science (Grant No. W8090303) and the Science Foundation of Yunnan province (Grant Nos. 2009BC018 and 2010CI019) and to Dr. Y. P. He, the knowledge Innovation Program of Chinese Academy of Sciences (KSCX1-YW- R-24), 973 Program (2006CB504200), Key Scientific and Techno- logical projects of Yunnan (2004NG12) to Dr. Y. T. Zheng. We would like to acknowledge MRC AIDS Research Project (UK) for providing cell lines and virus.
语种	英语
公开日期	2011-03-15
内容类型	期刊论文
源URL	[http://159.226.149.42:8088/handle/353002/6580]
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.Key Laboratory of Medicinal Chemistry for Natural Resource Ministry of Education, School of Chemical Science and Technology, Yunnan University, Kunming 650091, PR China 2.Laboratory of Molecular Immunopharmacology, Key Laboratory of Animal Models and Human Disease Mechanisms, Kunming Institute of Zoology, Chinese Academy of Sciences, Kunming 650223, PR China 3.Chemical Biology Laboratory, Center for Cancer Research, National Cancer Institute, Frederick, MD 21702, USA
推荐引用方式 GB/T 7714	He YP[*],Long J,Zhang SS,et al. Synthesis and biological evaluation of novel dihydro-aryl/alkylsulfanyl-cyclohexylmethyl-oxopyrimidines (S-DACOs) as high active anti-HIV agents[J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,2011,21(2):694-697.
APA	He YP[].,Long J.,Zhang SS.,Li C.,Lai CC.,...&Zheng YT[].(2011).Synthesis and biological evaluation of novel dihydro-aryl/alkylsulfanyl-cyclohexylmethyl-oxopyrimidines (S-DACOs) as high active anti-HIV agents.BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,21(2),694-697.
MLA	He YP[*],et al."Synthesis and biological evaluation of novel dihydro-aryl/alkylsulfanyl-cyclohexylmethyl-oxopyrimidines (S-DACOs) as high active anti-HIV agents".BIOORGANIC & MEDICINAL CHEMISTRY LETTERS 21.2(2011):694-697.