Synthesis and preliminary biological evaluation of Tc-99m(CO)(3)-labeled pegylated 2-nitroimidazoles
文献类型：期刊论文
| ; | |
| 作者 | Wang JJ(汪建军); Wang, JJ; Zheng, XB; Wu, WS; Yang, WJ; Liu, Y; Yang WJ(杨文江); 刘宇(多) |
| 刊名 | JOURNAL OF RADIOANALYTICAL AND NUCLEAR CHEMISTRY
 ; JOURNAL OF RADIOANALYTICAL AND NUCLEAR CHEMISTRY
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| 出版日期 | 2014 ; 2014 |
| 卷号 | 300期号:3页码:1013-1020 |
| 关键词 | [Tc-99m(CO)(3)](+) Label 2-nitroimidazole Pegylated Tumor hypoxia imaging [Tc-99m(CO)(3)](+) Label 2-nitroimidazole Pegylated Tumor hypoxia imaging |
| ISSN号 | 0236-5731 |
| DOI | 10.1007/s10967-014-3038-9 |
| 英文摘要 | 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.; 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. |
| 学科主题 | Chemistry; Nuclear Science & Technology ; Chemistry; Nuclear Science & Technology |
| 收录类别 | SCI |
| 电子版国际标准刊号 | 1588-2780 |
| 语种 | 英语 |
| WOS记录号 | WOS:000335673800014 ; WOS:000335673800014 |
| 公开日期 | 2016-05-03 |
| 源URL | [http://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, Synthesis and preliminary biological evaluation of Tc-99m(CO)(3)-labeled pegylated 2-nitroimidazoles[J]. JOURNAL OF RADIOANALYTICAL AND NUCLEAR CHEMISTRY, JOURNAL OF RADIOANALYTICAL AND NUCLEAR CHEMISTRY,2014, 2014,300, 300(3):1013-1020, 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. |
入库方式： OAI收割
来源：高能物理研究所
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