Synthesis of a Tyr-octreotate conjugated closo-carborane [HC2B10H10]: a potential compound for boron neutron capture therapy |
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Authors: | Esther SchirrmacherRalf Schirrmacher,Carmen BeckWalter Mier,Norbert TrautmanFrank Rö sch |
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Affiliation: | a Institute of Nuclear Chemistry, University of Mainz, D-55177 Mainz, Germany b Universitätsklinikum Heidelberg, Department of Nuclear Medicine, D-69120 Heidelberg, Germany |
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Abstract: | A novel Tyr3-octreotate conjugated closo-carborane as a potential compound for boron neutron capture therapy was obtained via Fmoc solid phase peptide synthesis. The boron cluster [C2B10H11] was introduced through the reaction of 6,9-bis(acetonitrile)decaborane and 5-hexynoic acid yielding a new closo-carborane conjugated carboxylic acid which was coupled subsequently with solid phase conjugated Tyr3-octreotate. The final boron-containing peptide was purified by preparative reverse phase HPLC and structural identity was proved applying MALDI-TOF mass spectrometry. |
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Keywords: | closo-carborane Tyr3-octreotate boron neutron capture therapy (BNCT) somatostatin receptor |
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