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

被引：15

作者：

Dapueto, Rosina ^{[2
,3
]}

Castelli, Romina ^{[3
]}

Fernandez, Marcelo ^{[3
]}

Chabalgoity, Jose A. ^{[1
]}

Moreno, Maria ^{[1
]}

Pablo Gambini, Juan ^{[4
]}

Cabral, Pablo ^{[1
]}

Porcal, Williams ^{[2
]}

机构：

[1] Univ Republica, Fac Med, Dept Desarrollo Biotecnol, Inst Higiene, Montevideo 11600, Uruguay

[2] Univ Republica, Fac Ciencia, Fac Quim, Lab Quim Organ, Montevideo 11400, Uruguay

[3] Univ Republica, Fac Ciencia, Lab Radiofarm, Ctr Invest Nucl, Montevideo 11400, Uruguay

[4] Univ Republica, Fac Med, Hosp Clin, Ctr Med Nucl, Montevideo 11600, Uruguay

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2011年 / 21卷 / 23期

关键词：

Glucose; 99m Technetium; Radiopharmaceutical; Melanoma; Tumor diagnostic; TC-99M;

D O I：

10.1016/j.bmcl.2011.09.106

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Glucose 9 and 2-deoxyglucose 10 were successfully synthesized and radiolabeled with [(99)mTc(CO)(3)(H2O)(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-Tc-99m complex could be considered as agents for melanoma diagnosis. (C) 2011 Elsevier Ltd. All rights reserved.

引用

页码：7102 / 7106

页数：5

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