CAS OpenIR  > 中科院上海应用物理研究所2011-2019年
Multi-substituted 8-aminoimidazo[1,2-a]pyrazines by Groebke-Blackburn-Bienayme reaction and their Hsp90 inhibitory activity
Ren, J; Yang, M; Liu, HC; Cao, DY; Chen, DQ; Li, J; Tang, L; He, JH; Chen, YL; Geng, MY; Xiong, B; Shen, JK
2015
Source PublicationORGANIC & BIOMOLECULAR CHEMISTRY
Volume13Issue:5Pages:1531—1535
Subtype期刊文献
AbstractUsing 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.
KeywordHeat-shock Proteins 3-component Condensation Discovery Heat-shock-protein-90 Identification Pyrazines Potent Chaperone
Indexed BySCI
Language英语
Document Type期刊论文
Identifierhttp://ir.sinap.ac.cn/handle/331007/24505
Collection中科院上海应用物理研究所2011-2019年
Recommended Citation
GB/T 7714
Ren, J,Yang, M,Liu, HC,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, J.,Yang, M.,Liu, HC.,Cao, DY.,Chen, DQ.,...&Shen, JK.(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, J,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.
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