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National Repository of Grey Literature 2 records found  Search took 0.00 seconds. 
Cyclam-based bifunctional ligands for selective metal ion complexation
 Hörnerová, Alžběta ; Kotek, Jan (advisor) ; Havlíček, David (referee)
Recently, the increasing demand for targeting radiopharmaceuticals motiva- tes the research of bifunctional ligands which should be able to coordinate radiometal ion into a stable complex and also contains avalaible functional group for binding to a biological vector. Especially the wide range of copper radionuclides is sparking interest for potencial applications in diagnosis and therapy of tumorous diseases. The ligands of the cyclam family are one of the most suitable for Cu(II) complexation. Relatively small number of unsymmetrically trans-disubstituted derivates has been prepared be- cause of difficult and non-trivial synthesis of these compounds. In this Diploma thesis a new orthogonal protection of cyclam is presented as a possible route of preparation of these compounds. Through this intermediate a ligand with methylenephosphonate and methylene(p-aminobenzyl)phosphinate pendant arms was synthesized, copper complexes of the ligand were prepared and their isomerism and stability/inertness were studied. Keywords: PET, SPECT, radiotherapy, copper, bifunctional ligands, orthogonal pro- tection of cyclam. 1
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Cyclam derivatives with coordinating bifunctional groups in 1,8 positions for selective copper(II) complexation
 Hörnerová, Alžběta ; Kotek, Jan (advisor) ; Vojtíšek, Pavel (referee)
Copper radionuclides are the object of increasing interest due to their advantageous properties for use in tumor diagnostics (PET, SPECT) and radiotherapy. In order to accomplish the best biodistribution the metal ion needs to be complexed by a suitable ligand attached to a biologically active molecule. The aim of this thesis is the synthesis of asymmetrically disubstituted derivatives of 1,4,8,11-tetraazacyclotetradecan (cyclam) with methylphosphonate and methylphosphinate pendant arms in 1,8 positions. Although the synthesis of designed ligands failed, the obtained knowledge will be used in further approaches of preparation of these compounds. Keywords: radiotherapy, SPECT, PET
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