Modification of poorly bioactive sinomenine into more potent immunosuppressive agents by embedding of drug-like fragments

	Modification of poorly bioactive sinomenine into more potent immunosuppressive agents by embedding of drug-like fragments
	Lou, YT; Zhou, HB; Zou, J; Yan, LC; Bi, EG; Sun, B; Yao, ZJ
刊名	TETRAHEDRON LETTERS
	2010
卷号	51 期号:3 页码:485-488
关键词	Sinomenine Alkaloid Drug fragment Modification Immunomodulating activity
通讯作者	Sun, B (reprint author), Chinese Acad Sci, Shanghai Inst Biol Sci, Shanghai Inst Biochem & Cell Biol, 219 Yueyong Rd, Shanghai 200031, Peoples R China.,bingsun@sib.ac.cn ; yaoz@mail.sioc.ac.cn
英文摘要	Embedment of drug-like heterocyclic moieties was Successfully employed in the novel modification of the readily available but poorly bioactive natural alkaloid sinomenine. Application of the newly proposed approach afforded a number of more potent sinomenine-like molecules with a significantly high hit rate. Among these new analogous, up to 500-fold increase of in vitro immunosuppressive activity was achieved. Further biological experiments of representative compound 4b indicated that it might inhibit NF-kappa B activation induced by TNF-alpha in a dose dependent way and showed remarkable in vivo treatment effects against the mouse experimental autoimmune uveoretinitis (EAU) disease models. (C) 2009 Elsevier Ltd. All rights reserved.
学科主题	Chemistry
类目[WOS]	Chemistry, Organic
关键词[WOS]	EXPERIMENTAL AUTOIMMUNE UVEORETINITIS ; CELLS ; MICE ; EXPRESSION ; MODEL ; EAU
收录类别	SCI
语种	英语
WOS记录号	WOS:000274477300006
内容类型	期刊论文
版本	出版稿
源URL	[http://202.127.25.143/handle/331003/985]
专题	上海生化细胞研究所_上海生科院生化细胞研究所
推荐引用方式 GB/T 7714	Lou, YT,Zhou, HB,Zou, J,et al. Modification of poorly bioactive sinomenine into more potent immunosuppressive agents by embedding of drug-like fragments[J]. TETRAHEDRON LETTERS,2010,51(3):485-488.
APA	Lou, YT.,Zhou, HB.,Zou, J.,Yan, LC.,Bi, EG.,...&Yao, ZJ.(2010).Modification of poorly bioactive sinomenine into more potent immunosuppressive agents by embedding of drug-like fragments.TETRAHEDRON LETTERS,51(3),485-488.
MLA	Lou, YT,et al."Modification of poorly bioactive sinomenine into more potent immunosuppressive agents by embedding of drug-like fragments".TETRAHEDRON LETTERS 51.3(2010):485-488.