Synthesis and preliminary biological evaluation of a technetium-99m labeled thymidine analog

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

“…, from 99m Tc-ANMdU to 99m Tc-NHT). However, in the present work the ratio of 99m Tc-TMHHA was samller than that of 99m Tc-TMHEA (see Table 3 ), and the both ratios of 99m Tc-TMHHA and 99m Tc-TMHEA were smaller than that of 99m Tc-NHT (4.41 ± 0.32, at 2 h post injection) [ 13 ]. This indicates that limitless extension of the carbon chain is not always beneficial to improve the uptake ratio of tumor to muscle.…”

“…The tumor uptake value was higher than that of muscle, and the uptake ratio of tumor to muscle was increased with time for 99m Tc-TMHEA and 99m Tc-TMHHA, respectively. In previous work of our group [ 12 , 13 ], it was found that the uptake ratio of tumor to muscle increases with the increasing carbon chain length between the thymidine and N 2 S 2 ligand ( i.e. , from 99m Tc-ANMdU to 99m Tc-NHT).…”

“…Therefore it is important to develop a 99m Tc labeled thymidine analog so as to provide the ideal characteristics needed for routine clinical studies [ 9 , 10 , 11 ]. In the previous work of our group, a series of technetium-99m labeled thymine derivatives have been prepared and their in vivo biological properties were systematically investigated [ 12 , 13 ]. It was found that the uptake ratio of tumor to muscle of 99m Tc-NHT was higher than that of 99m Tc-ANMdU, which means that uptake ratio of tumor to muscle maybe increase with increasing carbon chain length between the thymidine and N 2 S 2 ligand.…”

Radiochemistry

“…The tricarbonyl-technetium unit was used in the development of bifunctional chelators for the labelling of histidine derivatives, 117,118 in the preparation 119 of a potential brain perfusion imaging agent and in the synthesis of a labelled cRGD peptide. 120 Bisaminoethanethiol was used to chelate technetium in the preparation of a thymidine analog 121 and diphosphonic acid derivatives 122,123 have proved useful in the development of radiopharmaceuticals for bone imaging. Leukocytes have been labelled 124 with technetium-99m by the use of hexamethylpropylene amine oxime.…”