Synthesis and anti-HIV-1 activity of S-dihydro(alkyloxy)benzyloxypyrimidine derivatives

	Synthesis and anti-HIV-1 activity of S-dihydro(alkyloxy)benzyloxypyrimidine derivatives
	Rao ZK 1; Long J 2; Zhang SS 1; He M 1; Ou LC 1; Zheng YT2; He YP1; Li C 1; zhengyt@mail.kiz.ac.cn ; yphe@ynu.edu.cn
	2008
发表期刊	MONATSHEFTE FUR CHEMIE
ISSN	0026-9247
卷号	139 期号:8 页码:967-974
合作性质	其它
摘要	Several 2-heteroaryl-, 2-heteroarylcarbonylmethyl-, 2-arylcarbonylmethyl, and 2-arylethyl derivatives of S-dihydro(alkyloxy)benzyloxypyrimidines have been synthesized and the anti-HIV activities of these compounds were tested in C8166 cell and against RT enzyme. It was found that some of these compounds showed good activity against HIV-1 (EC(50) = 0.014-0.8 mu M) with low toxicity (CC(50) value of 222-564 mu M) and high selectivity (SI value of 278-37743). The structure-activity relationships (SAR) of these compounds have also been discussed.
关键词	Nnrtis S-dabos Antiviral Activity Hiv-1
资助者	This research was supported by the National Natural Science Foundation of China (Grant No. 30530179), the Natural Science Foundation of education office of Yunnan province (5Z0475C) to Dr. Y.P. He, the knowledge Innovation Program of Chinese Academy of Sciences (KSCX1-YW-R-24), 973 Program (2006CB504200), Key Scientific and Technological 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. ; This research was supported by the National Natural Science Foundation of China (Grant No. 30530179), the Natural Science Foundation of education office of Yunnan province (5Z0475C) to Dr. Y.P. He, the knowledge Innovation Program of Chinese Academy of Sciences (KSCX1-YW-R-24), 973 Program (2006CB504200), Key Scientific and Technological 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. ; This research was supported by the National Natural Science Foundation of China (Grant No. 30530179), the Natural Science Foundation of education office of Yunnan province (5Z0475C) to Dr. Y.P. He, the knowledge Innovation Program of Chinese Academy of Sciences (KSCX1-YW-R-24), 973 Program (2006CB504200), Key Scientific and Technological 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. ; This research was supported by the National Natural Science Foundation of China (Grant No. 30530179), the Natural Science Foundation of education office of Yunnan province (5Z0475C) to Dr. Y.P. He, the knowledge Innovation Program of Chinese Academy of Sciences (KSCX1-YW-R-24), 973 Program (2006CB504200), Key Scientific and Technological 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.
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收录类别	SCI
语种	英语
资助者	This research was supported by the National Natural Science Foundation of China (Grant No. 30530179), the Natural Science Foundation of education office of Yunnan province (5Z0475C) to Dr. Y.P. He, the knowledge Innovation Program of Chinese Academy of Sciences (KSCX1-YW-R-24), 973 Program (2006CB504200), Key Scientific and Technological 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. ; This research was supported by the National Natural Science Foundation of China (Grant No. 30530179), the Natural Science Foundation of education office of Yunnan province (5Z0475C) to Dr. Y.P. He, the knowledge Innovation Program of Chinese Academy of Sciences (KSCX1-YW-R-24), 973 Program (2006CB504200), Key Scientific and Technological 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. ; This research was supported by the National Natural Science Foundation of China (Grant No. 30530179), the Natural Science Foundation of education office of Yunnan province (5Z0475C) to Dr. Y.P. He, the knowledge Innovation Program of Chinese Academy of Sciences (KSCX1-YW-R-24), 973 Program (2006CB504200), Key Scientific and Technological 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. ; This research was supported by the National Natural Science Foundation of China (Grant No. 30530179), the Natural Science Foundation of education office of Yunnan province (5Z0475C) to Dr. Y.P. He, the knowledge Innovation Program of Chinese Academy of Sciences (KSCX1-YW-R-24), 973 Program (2006CB504200), Key Scientific and Technological 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.
文献类型	期刊论文
条目标识符	http://ir.kiz.ac.cn/handle/152453/4631
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	zhengyt@mail.kiz.ac.cn; yphe@ynu.edu.cn
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, People’s Republic of China 2.Laboratory of Molecular Immunopharmacology, Key Laboratory of Animal Models and Human Disease Mechanisms, Chinese Academy of Sciences, Kunming Institute of Zoology, Kunming, People’s Republic of China
推荐引用方式 GB/T 7714	Rao ZK,Long J,Zhang SS,et al. Synthesis and anti-HIV-1 activity of S-dihydro(alkyloxy)benzyloxypyrimidine derivatives[J]. MONATSHEFTE FUR CHEMIE,2008,139(8):967-974.
APA	Rao ZK.,Long J.,Zhang SS.,He M.,Ou LC.,...&yphe@ynu.edu.cn.(2008).Synthesis and anti-HIV-1 activity of S-dihydro(alkyloxy)benzyloxypyrimidine derivatives.MONATSHEFTE FUR CHEMIE,139(8),967-974.
MLA	Rao ZK,et al."Synthesis and anti-HIV-1 activity of S-dihydro(alkyloxy)benzyloxypyrimidine derivatives".MONATSHEFTE FUR CHEMIE 139.8(2008):967-974.

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