Functionalized thymidine derivatives as carriers for the γ-emitter technetium tricarbonyl moiety

被引：8

作者：

Alberto, Roger ^{[2
]}

N'Dongo, Harmel P. ^{[2
]}

Clericuzio, Marco ^{[1
]}

Bonetti, Samuele ^{[1
]}

Gabano, Elisabetta ^{[1
]}

Cassino, Claudio ^{[1
]}

Ravera, Mauro ^{[1
]}

Osella, Domenico ^{[1
]}

机构：

[1] Univ Piemonte Orientale Amedeo Avogadro, Dipartimento Sci Ambiente & Vita, I-15121 Alessandria, Italy

[2] Univ Zurich, Inst Anorgan Chem, CH-8057 Zurich, Switzerland

来源：

INORGANICA CHIMICA ACTA | 2009年 / 362卷 / 13期

关键词：

Single photon emission tomography (SPECT); Drug targeting and delivery; Thymidine; Technetium; Rhenium; IN-VITRO; BIOLOGICAL EVALUATION; 3-(CARBORANYLALKYL)THYMIDINES; PROLIFERATION; BIOMOLECULES; COMPLEXES; KINASE-1; VIVO;

D O I：

10.1016/j.ica.2009.06.054

中图分类号：

O61 [无机化学];

学科分类号：

070301 ; 081704 ;

摘要：

Nuclear medicine imaging of cell proliferation has gained broad interest in clinical oncology. A good tracer to image cell proliferation, possibly associated to tumour progression, should rapidly and specifically be incorporated into growing DNA. Following this idea, we have singled out thymidine as a potential biological carrier for delivery of the organometallic fragment [M(CO)(3)](+) (M = "cold" Re, gamma-emitter Tc-99m) to DNA. In the present paper we report the two-step synthesis of thymidine N-3 derivatives and their coordination complexes. Thymidine could be alkylated without protecting the sugar alcoholic functions. Methyl-2,2'-diaminodiethylamine thymidine derivative was quickly reacted with rhenium and technetium carbonyls in almost quantitative yield. The resulting Tc-99m complex represents a convenient radiopharmaceutical for single photon emission tomography (SPECT). (C) 2009 Elsevier B. V. All rights reserved.

引用

页码：4785 / 4790

页数：6

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