6533b82efe1ef96bd1293b16

RESEARCH PRODUCT

Synthesis of a Tyr3-octreotate conjugated closo-carborane [HC2B10H10]: a potential compound for boron neutron capture therapy

Frank RöschCarmen BeckWalter MierNorbert TrautmanEsther SchirrmacherRalf Schirrmacher

subject

inorganic chemicalschemistry.chemical_classificationOctreotateCarboxylic acidOrganic Chemistrychemistry.chemical_elementConjugated systemBiochemistryMedicinal chemistrychemistry.chemical_compoundchemistryDecaboraneDrug DiscoveryPeptide synthesisCarboraneAcetonitrileBoronNuclear chemistry

description

Abstract 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.

https://doi.org/10.1016/j.tetlet.2003.10.048