99(m)Tc/Re complexes bearing bisnitroimidazole or mononitroimidazole as potential bioreductive markers for tumor: Synthesis, physicochemical characterization and biological evaluation
文献类型：期刊论文
| 作者 | Mei, Lei; Wang, Yue; Chu, Taiwei |
| 刊名 | EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
 |
| 出版日期 | 2012-12-01 |
| 卷号 | 58页码:50-63 |
| 关键词 | Bisnitroimidazole Technetium Rhenium Tumor Hypoxia Biodistribution |
| ISSN号 | 0223-5234 |
| DOI | 10.1016/j.ejmech.2012.09.042 |
| 英文摘要 | Four monoamine-monoamide dithiol (MAMA) ligands containing two or one nitroimidazole moieties were synthesized and labeled with Tc-99m (labeling yield > 95%). The proposed structures of Tc-99m-complexes are identified by comparison with analogous Re-MAMA complexes. Tc-99m-MAMA complexes show better physicochemical characters than (TcO)-Tc-99m-(PnAO-1-(2-nitroimidazole)). Reduction potentials of nitro groups of the rhenium complexes are within the range for bioreductive compounds. As expected, biodistribution studies demonstrate that the 2-nitroimidazole complex shows better tumor-to-tissue ratios than 4-nitroimidazole analog for mononitroimidazole complexes, but not for MAMA-bisnitroimidazoles due to higher lipophilicity. Both the bisnitroimidazole compounds show rapider excretion, lower background activity in liver and higher tumor-to-tissue ratios than the mono-nitroimidazoles. Better biodistribution characteristic makes both the MAMA-bisnitroimidazole complexes, especially (TC)-T-99m-15, be potential tumor hypoxia marker. (C) 2012 Elsevier Masson SAS. All rights reserved. |
| 语种 | 英语 |
| WOS记录号 | WOS:000312745100006 |
| 出版者 | ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER |
| 源URL | [http://ir.iccas.ac.cn/handle/121111/49619]  |
| 专题 | 中国科学院化学研究所 |
| 通讯作者 | Chu, Taiwei |
| 作者单位 | Peking Univ, Beijing Natl Lab Mol Sci, Radiochem & Radiat Chem Key Lab Fundamental Sci, Coll Chem & Mol Engn, Beijing 100871, Peoples R China |
| 推荐引用方式 GB/T 7714 | Mei, Lei,Wang, Yue,Chu, Taiwei. 99(m)Tc/Re complexes bearing bisnitroimidazole or mononitroimidazole as potential bioreductive markers for tumor: Synthesis, physicochemical characterization and biological evaluation[J]. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,2012,58:50-63. |
| APA | Mei, Lei,Wang, Yue,&Chu, Taiwei.(2012).99(m)Tc/Re complexes bearing bisnitroimidazole or mononitroimidazole as potential bioreductive markers for tumor: Synthesis, physicochemical characterization and biological evaluation.EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,58,50-63. |
| MLA | Mei, Lei,et al."99(m)Tc/Re complexes bearing bisnitroimidazole or mononitroimidazole as potential bioreductive markers for tumor: Synthesis, physicochemical characterization and biological evaluation".EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY 58(2012):50-63. |
入库方式： OAI收割
来源：化学研究所
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