- Synthesis and characterization of novel benzovesamicol analogs
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Three new racemic vesamicol analogs were successfully prepared in good yields and high purity. All compounds were characterized by both IR and NMR spectroscopy. Compounds (±)-5 and (±)-6 showed a moderate lipophilicity compared with reference compounds IBVM and DRC140, respectively. However, the lipophilicity of DRC140 and (±)-9 showed very similar behaviors. TUeBITAK.
- Assaad, Thaer
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- Radiochemical synthesis and preliminary evaluation of anti-bladder cancer monoclonal antibody BDI-1 labeled with rhenium-188
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The anti-human bladder cancer monoclonal antibody BDI-1 was radio-labeled with rhenium-188 by direct labeling methods using SnCl2 as reductant and MDP as stannous stabilizer or by indirect method using NHS-ECM ester as bifunctional chelator. Radiochemical yields of 30 ± 7.23% and 87.4 ± 5.67% and radiochemical purity of more than 95% were achieved. The inmmunoreactive fraction was 58.7%. The results showed that radionuclide 188Re might be employed using the same labeling methodology with 99mTc labeling of BDI-1 for radiommunoimaging (RII) and radioimmunotherapy (RIT) and that may be useful in radioimmunodetection and RIT of human bladder carcinoma in vivo. Copyright
- Wang, Rongfu,Zhang, Chungli,Yu, Lizhang,Guo, Yifeng,Bai, Ying
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- Synthesis and characterization of the copper(ii) complexes of new N 2S2-donor macrocyclic ligands: Synthesis and in vivo evaluation of the 64Cu complexes
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The aim of this work was to prepare a novel class of 64Cu(ii) labeled complexes with the new macrocyclic ligands 1,10-dithia-4,7- diazacyclododecane-3,8-dicarboxylic acid (NEC-SE, 1), 1,10-dithia-4,7- diazacyclotridecane-3,8-dicarboxylic acid (NEC-SP, 2) and 1,10-dithia-4,7- diazacyclotetradecane-3,8-dicarboxylic acid, (NEC-SB, 3) to evaluate the usefulness of these macrocycles for potential utility as 64Cu(ii) chelators. The corresponding non-radioactive complexes [Cu(NEC-SE)] ·3H2O (4), [Cu(NEC-SP)]·3H2O (5) and [Cu(NEC-SB)] (6) were prepared and their 64Cu-analogs, [ 64Cu(NEC-SE)] (7) and [64Cu(NEC-SP)] (8) and [ 64Cu(NEC-SB)] (9) were produced in >98% radiochemical purity. Rats were injected with complex 7, 8 or 9 and were euthanized at 1, 4 and 24 h. All three complexes are cleared from the blood over the first hour following injection but there is poor clearance of this activity over 24 h. A similar pattern of retention was noted in the liver where the levels of activity in this tissue at 1 h are not statistically different from those at 24 h. Molecular mechanics and DFT studies were performed on the complexes in order to gain insight into the lower stability. The Royal Society of Chemistry 2009.
- Papini, Grazia,Alidori, Simone,Lewis, Jason S.,Reichert, David E.,Pellei, Maura,Lobbia, Giancarlo Gioia,Biddlecombe, Grainne B.,Anderson, Carolyn J.,Santini, Carlo
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- METHOD OF ENCAPSULATING METAL COMPLEX WITHIN LIPOSOMES
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An object of the present invention is to provide a method of producing liposome wherein a complex of a short half-life metallic radioactive nuclide such as 99mTc and CD is encapsulated, with radiochemical yield and purity enabling practical application. The present invention provides a method of producing a liposome wherein a complex of a short half-life metallic radioactive nuclide and ethylenedicysteine (CD) is encapsulated, which comprises mixing a complex of a short half-life metallic radioactive nuclide and N-[2-(1H-pyrrolylmethyl)]-N'-(4-penten-3-on-2)-ethane-1,2-diamine with an ethylenedicysteine (CD)-encapsulated liposome, and incubating the mixture.
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(2010/02/09)
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