Synthesis, tc-99m-labeling, and preliminary biological evaluation of dtpa-melphalan conjugates
文献类型：期刊论文
| 作者 | Wang, Jianjun1,2; Yang, Wenjiang2; Xue, Jinquan2; Zhang, Yanhua2; Liu, Yu2 |
| 刊名 | Journal of labelled compounds & radiopharmaceuticals
 |
| 出版日期 | 2017-12-01 |
| 卷号 | 60期号:14页码:659-665 |
| 关键词 | Tc-99m-labeled Bifunctional chelating agent Dtpa Melphalan Tumor imaging |
| ISSN号 | 0362-4803 |
| DOI | 10.1002/jlcr.3575 |
| 通讯作者 | Wang, jianjun(wangjj2016@ncepu.edu.cn) |
| 英文摘要 | Melphalan (mfl) is a typical nitrogen mustard for the treatment of many types of cancer. for the purpose to develop novel tc-99m-labeled tumor imaging agents with spect, mfl was directly labeled by tc-99m using diethylene triamine pentacetate acid (dtpa) as bifunctional chelating agent. the novel ligands were successfully synthesized by conjugation of dtpa to mfl to get monosubstituted dtpa-mfl and bis-substituted dtpa-2mfl. radiolabeling was performed in high yield to get tc-99m-dtpa-mfl and tc-99m-dtpa-2mfl, respectively, which were hydrophilic and stable at room temperature. the high initial tumor uptake with retention, good tumor/muscle ratios, and satisfactory scintigraphic images suggested the potential of tc-99m-dtpa-mfl and tc-99m-dtpa-2mfl for tumor imaging. however, the slow normal tissue clearance would be a great obstacle. further modification on the linker and/or tc-99m-chelate to improve the tumor targeting efficacy and in vivo kinetic profiles is currently in progress. |
| WOS关键词 | TUMOR IMAGING AGENT ; DNA ; RADIOPHARMACEUTICALS |
| WOS研究方向 | Biochemistry & Molecular Biology ; Pharmacology & Pharmacy ; Chemistry |
| WOS类目 | Biochemical Research Methods ; Chemistry, Medicinal ; Chemistry, Analytical |
| 语种 | 英语 |
| WOS记录号 | WOS:000418411800004 |
| 出版者 | WILEY |
| URI标识 | http://www.irgrid.ac.cn/handle/1471x/2177826 |
| 专题 | 高能物理研究所 |
| 通讯作者 | Wang, Jianjun |
| 作者单位 | 1.North China Elect Power Univ, Coll Environm Sci & Engn, Beijing 100206, Peoples R China 2.Chinese Acad Sci, Inst High Energy Phys, Div Nucl Technol & Applicat, Beijing, Peoples R China |
| 推荐引用方式 GB/T 7714 | Wang, Jianjun,Yang, Wenjiang,Xue, Jinquan,et al. Synthesis, tc-99m-labeling, and preliminary biological evaluation of dtpa-melphalan conjugates[J]. Journal of labelled compounds & radiopharmaceuticals,2017,60(14):659-665. |
| APA | Wang, Jianjun,Yang, Wenjiang,Xue, Jinquan,Zhang, Yanhua,&Liu, Yu.(2017).Synthesis, tc-99m-labeling, and preliminary biological evaluation of dtpa-melphalan conjugates.Journal of labelled compounds & radiopharmaceuticals,60(14),659-665. |
| MLA | Wang, Jianjun,et al."Synthesis, tc-99m-labeling, and preliminary biological evaluation of dtpa-melphalan conjugates".Journal of labelled compounds & radiopharmaceuticals 60.14(2017):659-665. |
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来源：高能物理研究所
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