Synthesis and Binding Affinity of Fluorine Containing NG-acyl and -sulfonyl BIBP3226 Derivatives: Ligands for the NPY Y1 Receptor

Autor: Maxine P. Roberts, Nigel A. Lengkeek, Herbert Herzog, Andrew Katsifis, I-Chieh J. Lee, Christopher J. R. Fookes, Ivan Greguric, Lei Zhang, Branko Dikic
Rok vydání: 2016
Předmět:
Zdroj: Australian Journal of Chemistry. 69:746
ISSN: 0004-9425
DOI: 10.1071/ch15569
Popis: The neuropeptide Y (NPY) receptors are abundant in a range of tumours hence are a molecular target for tumour imaging and therapy, particularly by the use of radiolabelled molecules. NG-Substituted derivatives of the NPY receptor antagonist, BIBP3226, were prepared aiming to improve its current usability and to incorporate a positron-emitting radioisotope for development in positron emission tomography (PET) radiopharmaceuticals. The BIBP3226 derivatives were prepared in seven steps while retaining the critically important amino acid chirality. The acyl derivative retained acceptable ligand binding, however the sulfonyl derivatives lost almost all binding affinity.
Databáze: OpenAIRE