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首页> 外文期刊>International Journal of Basic and Applied Sciences >Optimization of labeled 125I- pyrimidine derivative and its biological evaluation
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Optimization of labeled 125I- pyrimidine derivative and its biological evaluation

机译：标记的125I-嘧啶衍生物的优化及其生物学评价

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This study describe the organic synthesis of 2-iodobenzamido (2-N-nitrobenzen-5, 6, 7, 8 tetrahydrobenzothieno [2, 3-d]) pyrimidine -4-(3H) one as an example for some pyrimidine derivative used a new series of as potential cancer chemotherapeutic agents. The precursor derivative is ?-(2-iodobenzamido)-? - (4-nitrophenyl)-N- [3-ethoxy-carbonyl-4, 5, 6, 7-tetrahydrobenzothiophen-2-l] acrylic acid amide which react with hydrazine hydrate. The purification process was done via crystallization using solvent ethanol. The overall yield 78% the structure of the synthesized compound was confirmed by correct analytical and spectral data .Also, The synthesized compound was labeled with radioactive iodine -125 via nucleophilic substitution reaction ,in the presence cuprous chloride, the labeling process was carried out at 95oC for 60 min. the radiochemical yield was determined by using thin layer chromatography and the yield is equal to 80%.Preliminary in-vivo study was examined in normal mice were performed after intravenous injection through the tail vein and the data show the labeling compound was cleared quickly from most body organs. The radioiodinated compound showed high brain uptake .The results in this study suggest that radioiodinated pyrimidine derivative may be useful as cancer chemotherapeutic agents. Keywords : Pyrimidine Derivatives / Iodine -125/ Tissues Distribution.
机译：本研究描述了2-碘苯甲酰胺基（2-N-硝基苯甲-5、6、7、8四氢苯并噻吩并[2,3-d]）嘧啶-4-（3H）的有机合成，以一些嘧啶衍生物的实例为例。新系列作为潜在的癌症化学治疗剂。前体衍生物是β-（2-碘苯甲酰胺基）-β。与水合肼反应的-（4-硝基苯基）-N- [3-乙氧基-羰基-4、5、6、7-四氢苯并噻吩-2-l]丙烯酸酰胺。通过使用溶剂乙醇的结晶来完成纯化过程。正确的分析和光谱数据证实了合成化合物结构的总收率为78％。此外，在放射性亚铜的存在下，通过亲核取代反应用放射性碘-125标记了合成的化合物，在95oC持续60分钟。通过薄层色谱法测定放射化学产率，产率为80％。通过尾静脉静脉注射后对正常小鼠进行了初步的体内研究，数据表明标记化合物已从大多数小鼠中快速清除。身体器官。放射性碘化物显示出较高的脑摄取。本研究结果表明，放射性碘化物嘧啶衍生物可用作癌症的化学治疗剂。关键词：嘧啶衍生物/碘-125 /组织分布。

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