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放射性标记嘧啶碱基和嘧啶核苷在动物模型中的肿瘤摄取:VI. 1-(3'-[36Cl]-氯代、1-(3'-[82Br]-溴代和1-(3'-[123I]-碘代-3'-脱氧-β-D-阿拉伯呋喃糖基)尿嘧啶。

Tumor uptake of radiolabelled pyrimidine bases and pyrimidine nucleosides in animal models: VI. 1-(3'-[36Cl]-chloro-, 1-(3'-[82Br]-bromo- and 1-(3'-[123I]-Iodo-3'-deoxy-beta-D-arabinofuranosyl)uracil.

作者信息

Lee Y W, Mercer J R, Wiebe L I, Knaus E E

出版信息

Int J Appl Radiat Isot. 1984 Nov;35(11):1057-61. doi: 10.1016/0020-708x(84)90010-3.

DOI:10.1016/0020-708x(84)90010-3
PMID:6526522
Abstract

3'-Radiohalogenated (36Cl, 82Br and 123I) "arabino" pyrimidine nucleosides were evaluated as potential tumor diagnostic agents in tumor bearing animals. No preferential tissue uptake was observed. The compounds were excreted mainly unchanged in the urine. The 3'-[36Cl]- and 3'-[82Br]-3'-deoxyarabino nucleosides exhibited biliary uptake. The low uptake of injected radioactivity by the tumor was probably due to the combined effects of the lack of a C-3' hydroxyl group in the "ribo" configuration, the presence of a halogen, the structural rigidity imposed by the presence of a halogen and the short biological half-lives of the compounds.

摘要

对3'-放射性卤代(36Cl、82Br和123I)“阿拉伯糖型”嘧啶核苷作为荷瘤动物潜在肿瘤诊断剂进行了评估。未观察到优先的组织摄取。这些化合物主要以未改变的形式经尿液排泄。3'-[36Cl]-和3'-[82Br]-3'-脱氧阿拉伯糖核苷表现出胆汁摄取。肿瘤对注入放射性的低摄取可能是由于“核糖”构型中缺乏C-3'羟基、存在卤素、卤素的存在所导致的结构刚性以及化合物较短的生物半衰期等综合作用。

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