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


Alberto, R; N'Dongo, H W P; Clericuzio, M; Bonetti, S; Gabano, E; Cassino, C; Ravera, M; Osella, D (2009). Functionalized thymidine derivatives as carriers for the γ-emitter technetium tricarbonyl moiety. Inorganica Chimica Acta, 362(13):4785-4790.

Abstract

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, γ-emitter 99mTc) 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 99mTc complex represents a convenient radiopharmaceutical for single photon emission tomography (SPECT).

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, γ-emitter 99mTc) 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 99mTc complex represents a convenient radiopharmaceutical for single photon emission tomography (SPECT).

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4 citations in Web of Science®
4 citations in Scopus®
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Additional indexing

Item Type:Journal Article, refereed, original work
Communities & Collections:07 Faculty of Science > Department of Chemistry
Dewey Decimal Classification:540 Chemistry
Language:English
Date:2009
Deposited On:21 Jan 2010 19:03
Last Modified:05 Apr 2016 13:47
Publisher:Elsevier
ISSN:0020-1693
Publisher DOI:10.1016/j.ica.2009.06.054

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