Preparation and Preliminary Biological Evaluation of Novel (99m)Tc-Labelled Thymidine Analogs as Tumor Imaging Agents

Two kinds of novel thymidine derivatives, N-thymidine-yl-N′-methyl-N′-{N′′-[2-sulfanyl-(ethylamino)acetyl]-2-aminoethylsulfanyl-1-hexanamide}-ethanediamine (TMHEA) and N-thymidine-yl-N′-methyl-N′-{N′′-[2-sulfanyl-(ethylamino)acetyl]-2-aminoethylsulfanyl-1-hexanamide}-hexanediamine (TMHHA) were prepa...

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Detalles Bibliográficos
Autores principales: Lu, Chunxiong, Jiang, Quanfu, Tan, Cheng, Tang, Jie, Zhang, Jiankang
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2012
Materias:
Article
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6269068/
https://www.ncbi.nlm.nih.gov/pubmed/22801365
http://dx.doi.org/10.3390/molecules17078518
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author Lu, Chunxiong
Jiang, Quanfu
Tan, Cheng
Tang, Jie
Zhang, Jiankang
author_facet Lu, Chunxiong
Jiang, Quanfu
Tan, Cheng
Tang, Jie
Zhang, Jiankang
author_sort Lu, Chunxiong
collection PubMed
description Two kinds of novel thymidine derivatives, N-thymidine-yl-N′-methyl-N′-{N′′-[2-sulfanyl-(ethylamino)acetyl]-2-aminoethylsulfanyl-1-hexanamide}-ethanediamine (TMHEA) and N-thymidine-yl-N′-methyl-N′-{N′′-[2-sulfanyl-(ethylamino)acetyl]-2-aminoethylsulfanyl-1-hexanamide}-hexanediamine (TMHHA) were prepared and successfully labeled with (99m)Tc in high labeling yields. The in vitro stability and in vivo biodistribution of (99m)Tc-TMHEA and (99m)Tc-TMHHA were investigated and compared. The biodistribution studies indicate that the radiotracer (99m)Tc-TMHEA displays selective tumor uptake, suggesting it is a potential tumor imaging agent.
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spelling pubmed-62690682018-12-12 Preparation and Preliminary Biological Evaluation of Novel (99m)Tc-Labelled Thymidine Analogs as Tumor Imaging Agents Lu, Chunxiong Jiang, Quanfu Tan, Cheng Tang, Jie Zhang, Jiankang Molecules Article Two kinds of novel thymidine derivatives, N-thymidine-yl-N′-methyl-N′-{N′′-[2-sulfanyl-(ethylamino)acetyl]-2-aminoethylsulfanyl-1-hexanamide}-ethanediamine (TMHEA) and N-thymidine-yl-N′-methyl-N′-{N′′-[2-sulfanyl-(ethylamino)acetyl]-2-aminoethylsulfanyl-1-hexanamide}-hexanediamine (TMHHA) were prepared and successfully labeled with (99m)Tc in high labeling yields. The in vitro stability and in vivo biodistribution of (99m)Tc-TMHEA and (99m)Tc-TMHHA were investigated and compared. The biodistribution studies indicate that the radiotracer (99m)Tc-TMHEA displays selective tumor uptake, suggesting it is a potential tumor imaging agent. MDPI 2012-07-16 /pmc/articles/PMC6269068/ /pubmed/22801365 http://dx.doi.org/10.3390/molecules17078518 Text en © 2012 by the authors; licensee MDPI, Basel, Switzerland. http://creativecommons.org/licenses/by/3.0/ This article is an open-access article distributed under the terms and conditions of the Creative Commons Attribution license (http://creativecommons.org/licenses/by/3.0/).
spellingShingle Article
Lu, Chunxiong
Jiang, Quanfu
Tan, Cheng
Tang, Jie
Zhang, Jiankang
Preparation and Preliminary Biological Evaluation of Novel (99m)Tc-Labelled Thymidine Analogs as Tumor Imaging Agents
title Preparation and Preliminary Biological Evaluation of Novel (99m)Tc-Labelled Thymidine Analogs as Tumor Imaging Agents
title_full Preparation and Preliminary Biological Evaluation of Novel (99m)Tc-Labelled Thymidine Analogs as Tumor Imaging Agents
title_fullStr Preparation and Preliminary Biological Evaluation of Novel (99m)Tc-Labelled Thymidine Analogs as Tumor Imaging Agents
title_full_unstemmed Preparation and Preliminary Biological Evaluation of Novel (99m)Tc-Labelled Thymidine Analogs as Tumor Imaging Agents
title_short Preparation and Preliminary Biological Evaluation of Novel (99m)Tc-Labelled Thymidine Analogs as Tumor Imaging Agents
title_sort preparation and preliminary biological evaluation of novel (99m)tc-labelled thymidine analogs as tumor imaging agents
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6269068/
https://www.ncbi.nlm.nih.gov/pubmed/22801365
http://dx.doi.org/10.3390/molecules17078518
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