Structure-activity relationship study towards non-peptidic positron emission tomography (PET) radiotracer for gastrin releasing peptide receptors: Development of [

Autor:	Enza, Lacivita, Ermelinda, Lucente, Chantal, Kwizera, Ines F, Antunes, Mauro, Niso, Paola, De Giorgio, Roberto, Perrone, Nicola A, Colabufo, Philip H, Elsinga, Marcello, Leopoldo
Rok vydání:	2016
Předmět:	Fluorine Radioisotopes Indoles Phenylurea Compounds Tryptophan Stereoisomerism Ligands Rats Receptors Bombesin Structure-Activity Relationship Drug Stability Cell Line Tumor Positron-Emission Tomography Microsomes Liver Animals Humans Radiopharmaceuticals Oxidation-Reduction
Zdroj:	Bioorganicmedicinal chemistry. 25(1)
ISSN:	1464-3391
Popis:	Gastrin-releasing peptide receptors (GRP-Rs, also known as bombesin 2 receptors) are overexpressed in a variety of human cancers, including prostate cancer, and therefore they represent a promising target for in vivo imaging of tumors using positron emission tomography (PET). Structural modifications of the non-peptidic GRP-R antagonist PD-176252 ((S)-1a) led to the identification of the fluorinated analog (S)-3-(1H-indol-3-yl)-N-[1-[5-(2-fluoroethoxy)pyridin-2-yl]cyclohexylmethyl]-2-methyl-2-[3-(4-nitrophenyl)ureido]propionamide ((S)-1m) that showed high affinity and antagonistic properties for GRP-R. This antagonist was stable in rat plasma and towards microsomal oxidative metabolism in vitro. (S)-1m was successfully radiolabeled with fluorine-18 through a conventional radiochemistry procedure. [
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=pmid________::170fcf3ccb1d51a6b2a22606474efe6f https://pubmed.ncbi.nlm.nih.gov/27863916 Zobrazit plný text záznamu Full Text from ScienceDirect