Preparation and Preliminary Biological Evaluation of Novel 99mTc-Labelled Thymidine Analogs as Tumor Imaging Agents

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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 prepared and successfully labeled with (99m)Tc in high labeling yields. The in vitro stability and in ...

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Achieving a (99m)Tc labeled thymidine radiotracer for single photon emission tomography (SPECT) is considered to be of interest. In this study, four novel thymidine analogs, 6a, 6b, 6c and 6d, were successfully synthesized via "click reaction" route and then radiolabeled using a [(99m)Tc(CO)₃]⁺ core to prepare the corresponding (99m)Tc(CO)₃ complexes in high yields. These complexes were hydroph...

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Synthesis and Preliminary Evaluation of a New 99mTc Labeled Substance P Analogue as a Potential Tumor Imaging Agent

Neurokinin 1 receptors (NK1R) are overexpressed on several types of important human cancer cells. Substance P (SP) is the most specific endogenous ligand known for NK1Rs. Accordingly, a new SP analogue was synthesized and evaluated for detection of NK1R positive tumors. [6-hydrazinopyridine-3-carboxylic acid (HYNIC)-Tyr8-Met(O)11-SP] was synthesized and radiolabeled with 99mTc using ethylenedia...

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Synthesis and Preliminary Evaluation of a New 99mTc Labeled Substance P Analogue as a Potential Tumor Imaging Agent

Neurokinin 1 receptors (NK1R) are overexpressed on several types of important human cancer cells. Substance P (SP) is the most specific endogenous ligand known for NK1Rs. Accordingly, a new SP analogue was synthesized and evaluated for detection of NK1R positive tumors. [6-hydrazinopyridine-3-carboxylic acid (HYNIC)-Tyr8-Met(O)11-SP] was synthesized and radiolabeled with 99mTc using ethylenedia...

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Tumor Imaging with 99mTc-Labelled Antibody Fragmentst

Althoughthe labelling of proteins with was established in 1964 by McAfee, et al., this isotope has been avoided by most investigators for the labelling of antibodies for tumor localization. There are several reasons for this: (1)the half-life is only 6 hours while most previous radiolabelled antibody localization studies have shown that the required tumor-toblood ratio needed for tumor visualiz...

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ژورنال

عنوان ژورنال: Molecules

سال: 2012

ISSN: 1420-3049

DOI: 10.3390/molecules17078518