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以[99mTc(CO)3(H2O)3]+核为标记物的葡萄糖和脱氧葡萄糖衍生物的生物学评价作为潜在的黑色素瘤成像剂。

Biological evaluation of glucose and deoxyglucose derivatives radiolabeled with [99mTc(CO)3(H2O)3]+ core as potential melanoma imaging agents.

机构信息

Laboratorio de Química Orgánica, Igua 4225, Facultad de Ciencias-Facultad de Química, Universidad de la República, Montevideo, Uruguay.

出版信息

Bioorg Med Chem Lett. 2011 Dec 1;21(23):7102-6. doi: 10.1016/j.bmcl.2011.09.106. Epub 2011 Oct 1.

Abstract

Glucose 9 and 2-deoxyglucose 10 were successfully synthesized and radiolabeled with (99m)Tc(CO)(3)(H(2)0)(3) intermediate in high yield. The complexes were characterized by HPLC and its stability with histidine over time was challenged. Cell uptake and biodistribution studies in melanoma-bearing C57BL/6 mice were performed. Both compounds showed accumulation in tumor tissue with high tumor-to-muscle ratios. Thus, D-glucose- and D-2-deoxyglucose-(99m)Tc complex could be considered as agents for melanoma diagnosis.

摘要

成功合成了葡萄糖 9 和 2-脱氧葡萄糖 10,并通过 (99m)Tc(CO)(3)(H(2)0)(3) 中间体进行了高收率放射性标记。通过 HPLC 对配合物进行了表征,并考察了其与组氨酸随时间的稳定性。在携带黑色素瘤的 C57BL/6 小鼠中进行了细胞摄取和生物分布研究。两种化合物均在肿瘤组织中积累,具有较高的肿瘤与肌肉比值。因此,D-葡萄糖和 D-2-脱氧葡萄糖-(99m)Tc 配合物可被认为是用于黑色素瘤诊断的试剂。

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