198065-30-4Relevant academic research and scientific papers
Synthesis and biological evaluation of technetium-99m-labeled deoxyglucose derivatives as imaging agents for tumor
Chen, Xiangji,Li, Liang,Liu, Fei,Liu, Boli
, p. 5503 - 5506 (2006)
Three deoxyglucose (DG) derivatives, S-DG, MAG3-DG and MAMA-BA-DG, were synthesized and labeled successfully with high labeling yields and high radio-chemical purities. Biodistribution in tumor-bearing mice demonstrated that these three new su
Synthesis of sulfonamide conjugates of Cu(ii), Ga(iii), In(iii), Re(v) and Zn(ii) complexes: Carbonic anhydrase inhibition studies and cellular imaging investigations
Dilworth, Jonathan R.,Pascu, Sofia I.,Waghorn, Philip A.,Vullo, Daniela,Bayly, Simon R.,Christlieb, Martin,Sun, Xin,Supuran, Claudiu T.
, p. 4859 - 4873 (2015/03/18)
Carbonic anhydrase IX (CA IX) is currently generating great interest as a marker of tumour hypoxia and a potential chemotherapeutic target. In order to test the principle that a CA IX inhibitor could be used for targeting PET or SPECT metallic radioisotopes to tumours we have prepared a number of conjugates involving aryl-sulfonamides or an acetazolamide derivative linked to a range of copper, indium, rhenium, 99m-technetium and zinc complexes. Radiolabelled 64Cu and 99mTc analogues of the 'cold' Cu and some of the Re complexes were prepared in good radiochemical incorporation. Inhibition of various human carbonic anhydrase isoforms (I, II, IX and XII) was tested with the 'cold', non-radiolabelled complexes, and compared with an acetazolamide standard (AZA). The molecular structure of a new, tri-sulfonated porphyrin-labeled sulfonamide was determined using synchrotron X-ray crystallography. This journal is
Novel [99mTcN]2+ labeled EGFR inhibitors as potential radiotracers for single photon emission computed tomography (SPECT) tumor imaging
Zhao, Mingxia,Ning, Hongyu,Feng, Man,Li, Shilei,Chang, Jin,Qi, Chuanmin
, p. 5508 - 5521 (2014/06/10)
The epidermal growth factor receptor (EGFR) is overexpressed in many cancers, including breast, ovarian, endometrial and non-small cell lung cancer. An EGFR-specific imaging agent could facilitate clinical evaluation of primary tumors or metastases. To achieve this goal, 4-(2-aminoethylamino)-6,7- dimethoxyquinazoline (ADMQ) was synthesized based on a 4-aminoquinazoline core and then conjugated with N-mercapto-acetylglycine (MAG) and N- mercaptoacetyltriglycine (MAG3), respectively, to give compounds 1 and 2. The final complexes [99mTcN]-1 and [99mTcN]-2 were successfully obtained with radiochemical purities of >99% and >98% as measured by radio-HPLC. No decomposition of the two complexes at room temperature was observed over a period of 2 h. Their partition coefficients indicated they were hydrophilic and the electrophoresis results showed they were negatively charged. Biodistribution in tumor-bearing mice demonstrated that the two new complexes showed tumor accumulation, high tumor-tomuscle (T/M) ratios and fast clearance from blood and muscle. Between the two compounds, the 99mTcN-MAG3-ADMQ ([99mTcN]-2) showed the better characteristics, with the tumor/muscle and tumor/blood ratios reached 2.11 and 1.90 at 60 min post-injection, 4.20 and 1.10 at 120 min post-injection, suggesting it could be a promising radiotracer for SPECT tumor imaging.
Comparison of the labelling characteristics of mercaptoacetyltriglycine (MAG3) with different S-protective groups
Okarvi, Subhani M.,Adriaens, Paul,Verbruggen
, p. 853 - 874 (2007/10/03)
A number of different thiol protective groups have been synthesized and attached to mercaptoacetyltriglycine (MAG3) ligand. The newly made MAG3 analogues were labelled with 99mTc by direct labelling under alkaline condition and by stannous tartrate exchange labelling method. In the latter method, the amount of the ligand, reaction temperature and pH varied and their effects on the labelling efficiencies were studied. Radiochemical purities of 51% to 70%, 58% to 75% and 46% to 81% respectively, were obtained by radio-HPLC analysis for the studied MAG3 precursors when, 0.1 mg, 0.4 mg and 1.6 mg of the ligand was used and labelling was performed at both low temperature (70°C) and pH (pH 3). All the studied ligands were efficiently labelled with 99mTc (up to 99%) when heated for 10 min at pH 9 and 100°C. The labelling efficiency obtained by the direct labelling method for MAG3 analogues varied from 32% to 94% and was in all cases lower than after the exchange labelling at pH 9 and at 100°C. It was observed that the radiochemical purities can be improved significantly by heating the 'direct labelling mixture' at elevated temperature.
