Synthesis of a Tyr3-octreotate conjugated closo-carborane [HC2B10H10]: a potential compound for boron neutron capture therapy
- Resource Type
- Authors
- Frank Rösch; Carmen Beck; Walter Mier; Norbert Trautman; Esther Schirrmacher; Ralf Schirrmacher
- Source
- Tetrahedron Letters. 44:9143-9145
- Subject
- inorganic chemicals
chemistry.chemical_classification
Octreotate
Carboxylic acid
Organic Chemistry
chemistry.chemical_element
Conjugated system
Biochemistry
Medicinal chemistry
chemistry.chemical_compound
chemistry
Decaborane
Drug Discovery
Peptide synthesis
Carborane
Acetonitrile
Boron
Nuclear chemistry
- Language
- ISSN
- 0040-4039
A novel Tyr 3 -octreotate conjugated closo -carborane as a potential compound for boron neutron capture therapy was obtained via Fmoc solid phase peptide synthesis. The boron cluster [C 2 B 10 H 11 ] 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 Tyr 3 -octreotate. The final boron-containing peptide was purified by preparative reverse phase HPLC and structural identity was proved applying MALDI-TOF mass spectrometry.