Synthesis and biological evaluation of novel 99mTc-oxo and 99mTc-nitrido complexes with phenylalanine dithiocarbamate for tumor imaging

Zhu, Jingjing; Wang, Yue; Li, Zhenxiang; Fang, Si’an; Zhang, Junbo

doi:10.1007/s10967-014-3160-8

Cited by 13 publications

(9 citation statements)

References 20 publications

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“…In vitro stability of 99m Tc‐ AMD3465 in saline and mice serum were determined by TLC based on the method reported previously . To 0.4 mL of saline or mice serum, 0.1 mL of 99m Tc‐AMD3465 was added, and the mixture was incubated at 37°C for 30 minutes, 2 hours, and 4 hours.…”

Section: Methodsmentioning

confidence: 99%

Development of a novel ^99mTc‐labeled small molecular antagonist for CXCR4 positive tumor imaging

Zhang

You

Chen

et al. 2018

Labelled Comp Radiopharmac

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The chemokine receptor 4 (CXCR4) has been an attractive molecular target for tumor imaging, because it is overexpressed in many tumor types and involved in tumor progression and metastasis. The purpose of this study is to examine the CXCR4 targeting properties of Tc-labeled AMD3465, a small molecule antagonist of CXCR4. Tc-AMD3465 was prepared in high yield (>95%) and stable in mice serum at least for 4 hours. In vitro cell binding experiments were performed with Chinese hamster ovary (CHO), MCF-7 (breast cancer), and CHO-CXCR4 (CHO stably transfected to express CXCR4) cell lines. Small animal single photon emission computed tomography/computed tomography imaging studies in nude mice bearing MCF-7 and CHO xenografts showed that the uptakes of the radiotracer in MCF-7 tumors were significantly higher than those in the CXCR4-negative CHO tumors (P < 0.05), and the MCF-7 tumors uptake could be blocked with an excess of unlabeled AMD3465 (P < 0.05). These results suggested that Tc-AMD3465 could be a potential single photon emission computed tomography radiotracer for CXCR4 imaging.

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Section: Methodsmentioning

confidence: 99%

Development of a novel ^99mTc‐labeled small molecular antagonist for CXCR4 positive tumor imaging

Zhang

You

Chen

et al. 2018

Labelled Comp Radiopharmac

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“…The [ 99m TcO] 3+ core is isoelectronic with [ 99m TcN] 2+ , which has the ability to complex with the ciprofloxacin xanthate to form a stable labeled complex. By comparison, we prepared 99m TcO-CPF2XT through a ligand-exchange reaction by mixing CPF2XT and [ 99m TcO 4 ] − with the GH kit [ 22 ]. The log P value of 99m TcO-CPF2XT is −0.12 ± 0.05 and the bacteria binding value reduced by 58% after the excess of CPF2XT was added as an inhibitor.…”

Section: Discussionmentioning

confidence: 99%

Design, Preparation, and Evaluation of a Novel 99mTcN Complex of Ciprofloxacin Xanthate as a Potential Bacterial Infection Imaging Agent

et al. 2020

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In order to seek novel technetium-99m bacterial infection imaging agents, a ciprofloxacin xanthate (CPF2XT) was synthesized and radiolabeled with [99mTcN]2+ core to obtain the 99mTcN-CPF2XT complex, which exhibited high radiochemical purity, hydrophilicity, and good stability in vitro. The bacteria binding assay indicated that 99mTcN-CPF2XT had specificity to bacteria. A study of biodistribution in mice showed that 99mTcN-CPF2XT had a higher uptake in bacterial infection tissues than in turpentine-induced abscesses, indicating that it could distinguish bacterial infection from sterile inflammation. Compared to 99mTcN-CPFXDTC, the abscess/blood and abscess/muscle ratios of 99mTcN-CPF2XT were higher and the uptakes of 99mTcN-CPF2XT in the liver and lung were obviously decreased. The results suggested that 99mTcN-CPF2XT would be a potential bacterial infection imaging agent.

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“…The preparations of 99m TcO‐3’DTC‐TdR and 99m Tc(CO) 3 –3’DTC‐TdR were carried out according to the previously reported methods . The routes of the preparations were shown in Scheme .…”

Section: Methodsmentioning

confidence: 99%

Synthesis and biological evaluation of novel ^99mTc‐oxo and ^99mTc‐tricarbonyl complexes with C3′‐functionalized thymidine dithiocarbamate for tumor imaging

Duan

Gan

Song

et al. 2018

Applied Organom Chemis

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A novel C3′‐functionalized thymidine dithiocarbamate derivative (3’DTC‐TdR) was successfully synthesized and labelled using [99mTcO]3+ core and [99mTc(CO)3(H2O)3]+ core with high yields. The structures of the 99mTc complexes were verified by preparation and characterization of the corresponding stable rhenium complexes. Both of the complexes were lipophilic and stable in vitro. Cell internalization experiments indicated that the uptakes of 99mTcO‐3’DTC‐TdR were related to nucleoside transporters. Biodistribution of these complexes in mice bearing tumor showed that they had high tumor uptakes, good tumor/muscle ratios and tumor/blood ratios. Especially for 99mTcO‐3’DTC‐TdR, it exhibited the highest tumor/muscle ratio and tumor/blood ratio at 4 h post‐injection. SPECT/CT imaging studies indicated clear accumulation in tumor, suggesting 99mTcO‐3’DTC‐TdR would be a promising candidate for tumor imaging.

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Synthesis and biological evaluation of novel 99mTc-oxo and 99mTc-nitrido complexes with phenylalanine dithiocarbamate for tumor imaging

Cited by 13 publications

References 20 publications

Development of a novel ^99mTc‐labeled small molecular antagonist for CXCR4 positive tumor imaging

Development of a novel ^99mTc‐labeled small molecular antagonist for CXCR4 positive tumor imaging

Design, Preparation, and Evaluation of a Novel 99mTcN Complex of Ciprofloxacin Xanthate as a Potential Bacterial Infection Imaging Agent

Synthesis and biological evaluation of novel ^99mTc‐oxo and ^99mTc‐tricarbonyl complexes with C3′‐functionalized thymidine dithiocarbamate for tumor imaging

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Synthesis and biological evaluation of novel 99mTc-oxo and 99mTc-nitrido complexes with phenylalanine dithiocarbamate for tumor imaging

Cited by 13 publications

References 20 publications

Development of a novel 99mTc‐labeled small molecular antagonist for CXCR4 positive tumor imaging

Development of a novel 99mTc‐labeled small molecular antagonist for CXCR4 positive tumor imaging

Design, Preparation, and Evaluation of a Novel 99mTcN Complex of Ciprofloxacin Xanthate as a Potential Bacterial Infection Imaging Agent

Synthesis and biological evaluation of novel 99mTc‐oxo and 99mTc‐tricarbonyl complexes with C3′‐functionalized thymidine dithiocarbamate for tumor imaging

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Development of a novel ^99mTc‐labeled small molecular antagonist for CXCR4 positive tumor imaging

Development of a novel ^99mTc‐labeled small molecular antagonist for CXCR4 positive tumor imaging

Synthesis and biological evaluation of novel ^99mTc‐oxo and ^99mTc‐tricarbonyl complexes with C3′‐functionalized thymidine dithiocarbamate for tumor imaging