Synthesis and preliminary biological evaluation of Tc-99m(CO)(3)-labeled pegylated 2-nitroimidazoles

doi:10.1007/s10967-014-3038-9

IHEP OpenIR

	Synthesis and preliminary biological evaluation of Tc-99m(CO)(3)-labeled pegylated 2-nitroimidazoles
	Wang JJ(汪建军); Wang, JJ; Zheng, XB; Wu, WS; Yang, WJ; Liu, Y; Yang WJ(杨文江); 刘宇(多)
	2014
发表期刊	JOURNAL OF RADIOANALYTICAL AND NUCLEAR CHEMISTRY (IF:1.282[JCR-2016],1.219[5-Year])
ISSN	0236-5731
EISSN	1588-2780
卷号	300 期号:3 页码:1013-1020
摘要	This work reports the synthesis, radiolabeling and preliminary biodistribution results in tumor-bearing mice of Tc-99m(CO)(3)-labeled pegylated (PEG) 2-nitroimidazoles for tumor hypoxia imaging. The novel 2-nitroimidazole derivatives were successfully synthesized by conjugation of tridendate chelators to 2-nitroimidazole via PEG(3) linker. Radiolabeling was performed in high yield with [Tc-99m(CO)(3)](+) core to get cationic [Tc-99m(CO)(3)(BPA-PEG(3)-NIM)](+), neutral [Tc-99m(CO)(3)(AOPA-PEG(3)-NIM)] and anionic [Tc-99m(CO)(3)(IDA-PEG(3)-NIM)](-) respectively, all of which were hydrophilic and stable at room temperature. Biodistribution studies in tumor-bearing mice showed that Tc-99m(CO)(3)-labeled pegylated 2-nitroimidazoles accumulated in the tumor with low uptake. Tc-99m-chelate and charge had significant impact on partition coefficient, radiotracer tumor uptake and pharmacokinetic properties. The results indicate the need for synthetic modification of the parent 2-nitroimidazole derivatives and the Tc-99m-chelate with a view to improve the tumor targeting efficacy and in vivo kinetic profiles.
关键词	[Tc-99m(CO)(3)](+) Label 2-nitroimidazole Pegylated Tumor hypoxia imaging
学科领域	Chemistry; Nuclear Science & Technology
DOI	10.1007/s10967-014-3038-9
收录类别	SCI ; ADS
语种	英语
WOS记录号	WOS:000335673800014
ADS Bibcode	2014JRNC..300.1013W
ADS URL	https://ui.adsabs.harvard.edu/abs/2014JRNC..300.1013W
ADS引文	https://ui.adsabs.harvard.edu/abs/2014JRNC..300.1013W/citations
引用统计	正在获取... 被引频次：4 [ADS]
文献类型	期刊论文
条目标识符	https://ir.ihep.ac.cn/handle/311005/225159
专题	中国科学院高能物理研究所
推荐引用方式 GB/T 7714	Wang JJ,Wang, JJ,Zheng, XB,et al. Synthesis and preliminary biological evaluation of Tc-99m(CO)(3)-labeled pegylated 2-nitroimidazoles[J]. JOURNAL OF RADIOANALYTICAL AND NUCLEAR CHEMISTRY,2014,300(3):1013-1020.
APA	汪建军.,Wang, JJ.,Zheng, XB.,Wu, WS.,Yang, WJ.,...&刘宇.(2014).Synthesis and preliminary biological evaluation of Tc-99m(CO)(3)-labeled pegylated 2-nitroimidazoles.JOURNAL OF RADIOANALYTICAL AND NUCLEAR CHEMISTRY,300(3),1013-1020.
MLA	汪建军,et al."Synthesis and preliminary biological evaluation of Tc-99m(CO)(3)-labeled pegylated 2-nitroimidazoles".JOURNAL OF RADIOANALYTICAL AND NUCLEAR CHEMISTRY 300.3(2014):1013-1020.