Multi-substituted 8-aminoimidazo[1,2-a]pyrazines by Groebke-Blackburn-Bienayme reaction and their Hsp90 inhibitory activity

doi:10.1039/c4ob01865f

	Multi-substituted 8-aminoimidazo[1,2-a]pyrazines by Groebke-Blackburn-Bienayme reaction and their Hsp90 inhibitory activity
	Ren, Jing 1; Yang, Min 3; Liu, Hongchun2 ; Cao, Danyan 1; Chen, Danqi1 ; Li, Jian 3; Tang, Le 1; He, Jianhua 3; Chen, Yue-Lei1 ; Geng, Meiyu2
刊名	ORGANIC & BIOMOLECULAR CHEMISTRY
	2015
卷号	13 期号:5 页码:1531-1535
ISSN号	1477-0520
DOI	10.1039/c4ob01865f
文献子类	Article
英文摘要	Using a 2,3-diamino pyrazine substrate and yttrium triflate catalyst, various 2-alkyl and aryl substituted 3,8-diaminoimidazo[1,2-a]pyrazines were efficiently prepared through Groebke-Blackburn-Bienayme MCR. In particular, a novel 2-piperonyl 3,8-diaminoimidazo[1,2-a]pyrazine structure was prepared exclusively with this new method and was found to have moderate Hsp90 inhibitory activity. A crystalline complex with N-terminus ATP domain of Hsp90 and one of the new Hsp90 inhibitors was also obtained to elucidate the origin of activity of 2-piperonyl 3,8-diaminoimidazo[1,2-a]pyrazines.
资助项目	National Natural Science Foundation of China[81102306] ; National Natural Science Foundation of China[81273368] ; National Natural Science Foundation of China[81402850] ; National Science & Technology Major Project "Key New Drug Creation and Manufacturing Program", China[2012ZX09301001] ; National Science & Technology Major Project "Key New Drug Creation and Manufacturing Program", China[2014ZX09507-002]
WOS关键词	HEAT-SHOCK PROTEINS ; 3-COMPONENT CONDENSATION ; DISCOVERY ; HEAT-SHOCK-PROTEIN-90 ; IDENTIFICATION ; PYRAZINES ; POTENT ; CHAPERONE
WOS研究方向	Chemistry
语种	英语
出版者	ROYAL SOC CHEMISTRY
WOS记录号	WOS:000348212300031
内容类型	期刊论文
源URL	[http://119.78.100.183/handle/2S10ELR8/276769]
专题	药物化学研究室
通讯作者	Chen, Yue-Lei
作者单位	1.Chinese Acad Sci, Shanghai Inst Mat Med, Med Chem Dept, Shanghai 201203, Peoples R China; 2.Chinese Acad Sci, Shanghai Inst Mat Med, Div Antitumor Pharmacol, Shanghai 201203, Peoples R China 3.Chinese Acad Sci, Shanghai Inst Appl Phys, Shanghai 201203, Peoples R China;
推荐引用方式 GB/T 7714	Ren, Jing,Yang, Min,Liu, Hongchun,et al. Multi-substituted 8-aminoimidazo[1,2-a]pyrazines by Groebke-Blackburn-Bienayme reaction and their Hsp90 inhibitory activity[J]. ORGANIC & BIOMOLECULAR CHEMISTRY,2015,13(5):1531-1535.
APA	Ren, Jing.,Yang, Min.,Liu, Hongchun.,Cao, Danyan.,Chen, Danqi.,...&Shen, Jingkang.(2015).Multi-substituted 8-aminoimidazo[1,2-a]pyrazines by Groebke-Blackburn-Bienayme reaction and their Hsp90 inhibitory activity.ORGANIC & BIOMOLECULAR CHEMISTRY,13(5),1531-1535.
MLA	Ren, Jing,et al."Multi-substituted 8-aminoimidazo[1,2-a]pyrazines by Groebke-Blackburn-Bienayme reaction and their Hsp90 inhibitory activity".ORGANIC & BIOMOLECULAR CHEMISTRY 13.5(2015):1531-1535.