ISBN: 978-83-60043-10-3 - eurobic9

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Eurobic9, 2-6 September, 2008, Wrocław, Poland P55. Fac-Tc(Co)3 + And Fac-Re(Co)3 + Complexed by Histidine Derivatives - Potential Precursors of Radiopharmaceuticals L. Fuks a , E. Gniazdowska a , D. Papagiannopoulou b , P. Kozminski a , M. Papadopoulos c , M. Pelecanou c , I. Pirmettis c , C. Raptopoulou c , N. Sadlej-Sosnowska d , C. Tsoukalas c a Institute of Nuclear Chemistry and Technology, Warsaw, Poland e-mail: egniazdo@ichtj.waw.pl b School of Pharmacy, Aristotle University, Thessaloniki, Greece c National Centre of Scientific Research "DEMOKRITOS, Athens, Greece d National Medicines Institute, Warsaw, Poland Studies on the Tc(CO)3 + and Re(CO)3 + complexes in the last years have received special momentum since they give chance to prepare a series of novel radiopharmaceuticals [1]. Kinetic inertness of the tricarbonylrhenium(I) core containing cation of the d6 electronic configuration gives ground for the interest in its complexes, especially those obtained by substitution of two or three labile water molecules by bi- or tridentate chelating ligands. The aim of our studies is to find novel ligands, which form stable complexes with Tc(CO)3 + and Re(CO)3 + , that after conjugation to a biomolecule can be used for the development of 2 nd generation targeted radiopharmaceuticals. In the present paper we describe the synthesis and characterization of novel [Tc/Re(SNO)(CO)3] complexes where SNO is the 4-methoxybenzyl derivative of the 3-(1H-imidazol-4-yl)-2-mercaptopropanoic acid - a tridentate SNO ligand, synthesized from L-histidine. The IR spectrum of the [Re(SNO)(CO)3] complex indicates the characteristic bands of three facially coordinated CO groups. 1 H NMR studies show typical pattern of diasterotopic protons of the SNO backbone after complexation. X ray analysis of the complex shows octahedral structure with SNO ligand coordinated in a tripodal fashion. The presence of complex diasteromers was also explored by quantum chemical calculations that resulted in two potential configurations. Quantum chemical calculations have shown that they can be related to different complex structures with comparable energy (∆ ≈ 0.3 and 0.4 kcal/mol for Tc I and Re I respectively). Successful labeling of the SNO ligand with suitable fac-[ 99m Tc/ 188 Re(CO)3] + cores led to the formation of stable complexes at tracer level, indicating the suitability of this system for the development of novel radiopharmaceuticals. Fig.: cis- and trans-configurations (left and right, respectively) of ligand complexing the Re I (CO)3 + moiety. Conclusion: 3-(1H-imidazol-4-yl)-2-[(4-methoxybenzyl)thio]propanoic acid is a potent chelator for the fac- [ 99m Tc/ 188 Re(CO)3] + core and it could be applied for the design of novel bioactive fac-[ 99m Tc/ 188 Re(SNO)(CO)3] complexes - potential diagnostic or therapeutic radiopharmaceuticals, respectively. Acknowledgement Part of the work was performed within the Maria Curie Transfer of Knowledge training contract MTKD-CT- 2004-509224 (POL-RAD-PHARM: Chemical studies for design and production of new radiopharmaceuticals). References: [1] U. Abram, R Alberto, Technetium and Rhenium - Coordination Chemistry and Nuclear Medical Applications. J. Brazil. Chem. Soc., 2006, 17(8), 1486-1500. _____________________________________________________________________ 174
Eurobic9, 2-6 September, 2008, Wrocław, Poland P56. Complexes Containing the [99mTc(CO)3] + Core for the Targeted Radiotherapy L. Fuks a , K. Kothari a , M. Neves b a Institute of Nuclear Chemistry and Technology, Dorodna 16, 03-195, Warsaw, Poland e-mail: lfuks@ichtj.waw.pl b Technological and Nuclear Institute (ITN), Sacavem, Portugal 99m Tc is the radionuclide of choice for nuclear medicine imaging by SPECT. Because of the nuclear properties, complexes containing the monovalent 99m Tc(CO)3 + core and chelating organic ligands received special attention as radiopharmaceutical precursors [1]. The aim of this study is to find novel ligands, which form stable complexes with the Tc(CO)3 + cation and after further functionalization could serve as precursors for the synthesis of radiopharmaceuticals of the 2 nd generation. In the presentation we show our preliminary results on application of the tricarbonyltechnetium(I) complexes as therapeutic agents. Recently it was found, that technetium-99m nuclide is an Auger electron emitter and if located in the close proximity of the cancer cell nucleus can induce the DNA strand breaks [2]. Such requirements fulfill group of compounds being so called ‘2+1' or ‘3+0' complexes (see, Scheme 1).Please prepare your abstract in English language. Leave 2.5 cm (top), 2.5 cm (bottom), 2.5 cm (left) and 2.5 cm (right) margins on the A4 page. Scheme 1. 99mTc(CO)3+ ‘2+1' complex containing the biguanide ligand Presented work describes our recent studies on rhenium (non radioactive congener of technetium) and technetium-99m complexes with the biguanide and thiourea derivatives as the ligands in order to prepare new agents for targeted radiotherapy. Acknowledgement: The work was undertaken within the Polish-Portuguese bilateral scientific agreement between the Institute of Nuclear Chemistry and Technology and Technological and Nuclear Institute (ITN) financed by Polish and Portuguese Ministries of Science and Higher Education. Polish Ministery of Science and Higher Education is also acknowledged for the grant 122/N-Portugal/2008/0. References: [1]. U. Abram, R Alberto, Technetium and rhenium - coordination chemistry and nuclear medical applications, J. Brazil. Chem. Soc., 2006, 17(8), 1486-1500. [2]. (a) P. Haefliger, N. Agorastos, A. Renard, G. Giambonini-Brugnoli, C. Marty, R. Alberto, Cell uptake and radiotoxicity studies of an nuclear localization signal peptide-intercalator conjugate labeled with [ 99m Tc(CO)3] + , Bioconjugate chemistry, 2005, 16(3), 582-587; (b) F. Marques, A. Paulo, M.P. Campello, S. Lacerda, R.F. Vitor, L. Gano, R. Delgado, I. Santos, Radiopharmaceuticals for targeted radiotherapy, Rad. Prot. Dosim., 2005, 116(1-4 Pt. 2), 601-604. _____________________________________________________________________ 175
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ISBN: 978-83-60043-10-3 - eurobic9

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